N-3 substituted TSAO derivatives as a probe to explore the dimeric interface of HIV-1 reverse transcriptase.
|
Balzarini J
|
|
Nucleosides, nucleotides & nucleic acids
|
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: Synthesis, biological investigation and molecular modeling studies.
|
Balzarini J
|
2013
|
Bioorganic & medicinal chemistry
|
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
|
Balzarini J
|
2013
|
Bioorganic & medicinal chemistry letters
|
Design, Synthesis, and Biological Evaluation of Novel 3,5-Disubstituted-1,2,6-Thiadiazine-1,1-Dione Derivatives as HIV-1 NNRTIs.
|
Balzarini J
|
2013
|
Chemical biology & drug design
|
A Multi-targeted Drug Candidate with Dual Anti-HIV and Anti-HSV Activity.
|
Balzarini J
|
2013
|
PLoS pathogens
|
Discovery of Piperidine-Linked Pyridine Analogues as Potent Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors.
|
Balzarini J
|
2013
|
ChemMedChem
|
N(1),N(3)-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
|
Balzarini J
|
2013
|
Bioorganic & medicinal chemistry
|
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
|
Balzarini J
|
2013
|
Bioorganic & medicinal chemistry
|
Recent advances in thymidine kinase 2 (TK2) inhibitors and new perspectives for potential applications.
|
Balzarini J
|
2012
|
Current pharmaceutical design
|
Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
|
Balzarini J
|
2012
|
European journal of medicinal chemistry
|
Arylazolylthioacetanilide. Part 11: Design, Synthesis and Biological Evaluation of 1,2,4-Triazole Thioacetanilide Derivatives as Novel Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors.
|
Balzarini J
|
2012
|
Medicinal chemistry (Shāriqah (United Arab Emirates))
|
In vitro-selected drug-resistant varicella-zoster virus mutants in the thymidine kinase and DNA polymerase genes yield novel phenotype-genotype associations and highlight differences between antiherpesvirus drugs.
|
Balzarini J
|
2012
|
Journal of virology
|
Potential of carbohydrate-binding agents as therapeutics against enveloped viruses.
|
Balzarini J
|
2012
|
Medicinal research reviews
|
Exploiting the anti-HIV-1 activity of acyclovir: suppression of primary and drug-resistant HIV isolates and potentiation of the activity by ribavirin.
|
Balzarini J
|
2012
|
Antimicrobial agents and chemotherapy
|
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
|
Balzarini J
|
2012
|
European journal of medicinal chemistry
|
Topical tenofovir, a microbicide effective against HIV, inhibits herpes simplex virus-2 replication.
|
Balzarini J
|
2011
|
Cell host & microbe
|
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
|
Balzarini J
|
2011
|
Journal of medicinal chemistry
|
Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides.
|
Balzarini J
|
2011
|
Antiviral research
|
Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket.
|
Balzarini J
|
2011
|
Journal of medicinal chemistry
|
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
|
Balzarini J
|
2011
|
Bioorganic & medicinal chemistry
|
Synthesis and anti-HIV activity of aryl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazones as potent non-nucleoside reverse transcriptase inhibitors.
|
Balzarini J
|
2011
|
ChemMedChem
|
Novel antiviral C5-substituted pyrimidine acyclic nucleoside phosphonates selected as human thymidylate kinase substrates.
|
Balzarini J
|
2011
|
Journal of medicinal chemistry
|
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
|
Balzarini J
|
2010
|
Bioorganic & medicinal chemistry
|
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
|
Balzarini J
|
2010
|
Bioorganic & medicinal chemistry
|
Lead optimization of diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
|
Balzarini J
|
2010
|
ChemMedChem
|
The acyclic 2,4-diaminopyrimidine nucleoside phosphonate acts as a purine mimetic in HIV-1 reverse transcriptase DNA polymerization.
|
Balzarini J
|
2010
|
The Journal of biological chemistry
|
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
|
Balzarini J
|
2010
|
Bioorganic & medicinal chemistry
|
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
|
Balzarini J
|
2009
|
Journal of medicinal chemistry
|
Mechanisms associated with HIV-1 resistance to acyclovir by the V75I mutation in reverse transcriptase.
|
Balzarini J
|
2009
|
The Journal of biological chemistry
|
Synthesis and in vitro anti-HIV evaluation of a new series of 6-arylmethyl-substituted S-DABOs as potential non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
Balzarini J
|
2009
|
European journal of medicinal chemistry
|
The application of phosphoramidate protide technology to acyclovir confers anti-HIV inhibition.
|
Balzarini J
|
2009
|
Journal of medicinal chemistry
|
Design, synthesis, and SAR of naphthyl-substituted Diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
|
Balzarini J
|
2009
|
ChemMedChem
|
Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.
|
Balzarini J
|
2009
|
Yao xue xue bao = Acta pharmaceutica Sinica
|
Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 13: synthesis of fluorine-containing diaryltriazine derivatives for in vitro anti-HIV evaluation against wild-type strain.
|
Balzarini J
|
2009
|
Chemistry & biodiversity
|
Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: structural modulations of diaryltriazines with potent anti-HIV activity.
|
Balzarini J
|
2008
|
European journal of medicinal chemistry
|
Acyclovir is activated into a HIV-1 reverse transcriptase inhibitor in herpesvirus-infected human tissues.
|
Balzarini J
|
2008
|
Cell Host Microbe
|
Non-nucleoside HIV-1 reverse-transcriptase inhibitors. Part 10. Synthesis and anti-HIV activity of 5-alkyl-6-(1-naphthylmethyl)pyrimidin-4(3H)-ones with a mono- or disubstituted 2-amino function as novel 'dihydro-alkoxy-benzyl-oxopyrimidine' (DABO) analogues.
|
Balzarini J
|
2008
|
Chemistry & biodiversity
|
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
Balzarini J
|
2008
|
Bioorganic & medicinal chemistry
|
Activity of the small modified amino acid alpha-hydroxy glycineamide on in vitro and in vivo human immunodeficiency virus type 1 capsid assembly and infectivity.
|
Balzarini J
|
2008
|
Antimicrobial agents and chemotherapy
|
4"-Benzoylureido-TSAO derivatives as potent and selective non-nucleoside HCMV inhibitors. Structure-activity relationship and mechanism of antiviral action.
|
Balzarini J
|
2008
|
Journal of medicinal chemistry
|
Synthesis and anti-HIV activity evaluation of 1-[(alkenyl or alkynyl or alkyloxy)methyl]-5-alkyl-6-(1-naphthoyl)-2,4-pyrimidinediones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
Balzarini J
|
2007
|
European journal of medicinal chemistry
|
Novel non-nucleoside human cytomegalovirus inhibitors based upon TSAO nucleoside derivatives: structure-activity relationships.
|
Balzarini J
|
2007
|
Nucleosides, nucleotides & nucleic acids
|
Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and HCMV.
|
Balzarini J
|
2007
|
Nucleosides, nucleotides & nucleic acids
|
Comparative evaluation of the activity of antivirals towards feline immunodeficiency virus in different cell culture systems.
|
Balzarini J
|
2007
|
Antiviral research
|
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
|
Balzarini J
|
2007
|
Bioorganic & medicinal chemistry letters
|
Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or alpha-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
Balzarini J
|
2007
|
Journal of medicinal chemistry
|
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
|
Balzarini J
|
2007
|
European journal of medicinal chemistry
|
Synthesis and anti-HIV-1 and anti-HCMV activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil derivatives.
|
Balzarini J
|
2006
|
Chemical & pharmaceutical bulletin
|
Therapeutic strategies towards HIV-1 infection in macrophages.
|
Balzarini J
|
2006
|
Antiviral research
|
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization.
|
Balzarini J
|
2006
|
Journal of medicinal chemistry
|
Non-nucleoside HIV-1 reverse transcriptase inhibitors, Part 7. Synthesis, antiviral activity, and 3D-QSAR investigations of novel 6-(1-naphthoyl) HEPT analogues.
|
Balzarini J
|
2006
|
Chemical & pharmaceutical bulletin
|
Nonnucleoside HIV-1 reverse-transcriptase inhibitors, part 5. Synthesis and anti-HIV-1 activity of novel 6-naphthylthio HEPT analogues.
|
Balzarini J
|
2005
|
Chemical & pharmaceutical bulletin
|
Non-nucleoside HIV reverse transcriptase inhibitors, Part 6[1]: synthesis and anti-HIV activity of novel 2-[(arylcarbonylmethyl)thio]-6-arylthio DABO analogues.
|
Balzarini J
|
2005
|
Archiv der Pharmazie
|
High sequence conservation of human immunodeficiency virus type 1 reverse transcriptase under drug pressure despite the continuous appearance of mutations.
|
Balzarini J
|
2005
|
Journal of virology
|
First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication.
|
Balzarini J
|
2005
|
Journal of medicinal chemistry
|
The role of Thr139 in the human immunodeficiency virus type 1 reverse transcriptase sensitivity to (+)-calanolide A.
|
Balzarini J
|
2005
|
Molecular pharmacology
|
The molecular basis of resilience to the effect of the Lys103Asn mutation in non-nucleoside HIV-1 reverse transcriptase inhibitors studied by targeted molecular dynamics simulations.
|
Balzarini J
|
2005
|
Journal of the American Chemical Society
|
The N137 and P140 amino acids in the p51 and the P95 amino acid in the p66 subunit of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase are instrumental to maintain catalytic activity and to design new classes of anti-HIV-1 drugs.
|
Balzarini J
|
2005
|
FEBS letters
|
The amino acid Asn136 in HIV-1 reverse transcriptase (RT) maintains efficient association of both RT subunits and enables the rational design of novel RT inhibitors.
|
Balzarini J
|
2005
|
Molecular pharmacology
|
Susceptibilities of several clinical varicella-zoster virus (VZV) isolates and drug-resistant VZV strains to bicyclic furano pyrimidine nucleosides.
|
Balzarini J
|
2005
|
Antimicrobial agents and chemotherapy
|
Antiadenovirus activities of several classes of nucleoside and nucleotide analogues.
|
Balzarini J
|
2005
|
Antimicrobial agents and chemotherapy
|
Marked depletion of glycosylation sites in HIV-1 gp120 under selection pressure by the mannose-specific plant lectins of Hippeastrum hybrid and Galanthus nivalis.
|
Balzarini J
|
2005
|
Molecular pharmacology
|
Pyridine N-oxide derivatives: unusual anti-HIV compounds with multiple mechanisms of antiviral action.
|
Balzarini J
|
2005
|
The Journal of antimicrobial chemotherapy
|
Current status of the non-nucleoside reverse transcriptase inhibitors of human immunodeficiency virus type 1.
|
Balzarini J
|
2004
|
Current topics in medicinal chemistry
|
In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides.
|
Balzarini J
|
2004
|
Antimicrobial agents and chemotherapy
|
The phenylmethylthiazolylthiourea nonnucleoside reverse transcriptase (RT) inhibitor MSK-076 selects for a resistance mutation in the active site of human immunodeficiency virus type 2 RT.
|
Balzarini J
|
2004
|
Journal of virology
|
Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors.
|
Balzarini J
|
2004
|
Molecular pharmacology
|
Nonnucleoside HIV-1 reverse transcriptase inhibitors; part 3. Synthesis and antiviral activity of 5-alkyl-2-[(aryl and alkyloxyl-carbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones.
|
Balzarini J
|
2004
|
Bioorganic chemistry
|
2-(2,6-Dihalophenyl)-3-(pyrimidin-2-yl)-1,3-thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
Balzarini J
|
2004
|
Antiviral research
|
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
|
Balzarini J
|
2004
|
Bioorganic & medicinal chemistry letters
|
Antiviral profile of HIV inhibitors in macrophages: implications for therapy.
|
Balzarini J
|
2004
|
Current topics in medicinal chemistry
|
TSAO compounds: the comprehensive story of a unique family of HIV-1 specific inhibitors of reverse transcriptase.
|
Balzarini J
|
2004
|
Current topics in medicinal chemistry
|
Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
|
Balzarini J
|
2004
|
Farmaco (Società chimica italiana : 1989)
|
Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV.
|
Balzarini J
|
2003
|
Antiviral chemistry & chemotherapy
|
Structure-activity relationship studies on a novel family of specific HIV-1 reverse transcriptase inhibitors.
|
Balzarini J
|
2003
|
Antiviral chemistry & chemotherapy
|
A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude.
|
Balzarini J
|
2003
|
Journal of medicinal chemistry
|
N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action.
|
Balzarini J
|
2003
|
Journal of medicinal chemistry
|
Characterization of the catalytic subunit of the human herpesvirus 6 (HHV-6) DNA polymerase expressed in an in vitro transcription/translation assay.
|
Balzarini J
|
2003
|
Nucleosides, nucleotides & nucleic acids
|
Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription.
|
Balzarini J
|
2003
|
Journal of medicinal chemistry
|
Nonnucleoside HIV-1 reverse transcriptase inhibitors: Part I. Synthesis and structure-activity relationship of 1-alkoxymethyl-5-alkyl-6-naphthylmethyl uracils as HEPT analogues.
|
Balzarini J
|
2003
|
Chemical & pharmaceutical bulletin
|
Inhibition of human immunodeficiency virus by a new class of pyridine oxide derivatives.
|
Balzarini J
|
2003
|
Antimicrobial agents and chemotherapy
|
Novel human immunodeficiency virus (HIV) inhibitors that have a dual mode of anti-HIV action.
|
Balzarini J
|
2003
|
Antimicrobial agents and chemotherapy
|
Synthesis, solution conformation and anti-HIV activity of novel 3'-substituted-2',3'-dideoxy-5-hydroxymethyluridines and their 4,5-substituted analogues.
|
Balzarini J
|
2003
|
Antiviral chemistry & chemotherapy
|
Synthesis and antiviral activity of some 5'-N-phthaloyl-3'-azido-2',3'-dideoxythymidine analogues.
|
Balzarini J
|
2003
|
Antiviral chemistry & chemotherapy
|
Macrophages and HIV infection: therapeutical approaches toward this strategic virus reservoir.
|
Balzarini J
|
2002
|
Antiviral research
|
Metabolic activation of nucleoside and nucleotide reverse transcriptase inhibitors in dendritic and Langerhans cells.
|
Balzarini J
|
2002
|
AIDS (London, England)
|
Activity of reverse transcriptase inhibitors in monocyte-derived dendritic cells: a possible in vitro model for postexposure prophylaxis of sexual HIV transmission.
|
Balzarini J
|
2002
|
AIDS research and human retroviruses
|
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.
|
Balzarini J
|
2002
|
Journal of medicinal chemistry
|
Chemotherapy of varicella-zoster virus by a novel class of highly specific anti-VZV bicyclic pyrimidine nucleosides.
|
Balzarini J
|
2002
|
Biochimica et biophysica acta
|
Chimeric human immunodeficiency virus type 1 and feline immunodeficiency virus reverse transcriptases: role of the subunits in resistance/sensitivity to non-nucleoside reverse transcriptase inhibitors.
|
Balzarini J
|
2002
|
Molecular pharmacology
|
Exploitation of the low fidelity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase and the nucleotide composition bias in the HIV-1 genome to alter the drug resistance development of HIV.
|
Balzarini J
|
2001
|
Journal of virology
|
Synthesis, biological activity, pharmacokinetic properties and molecular modelling studies of novel 1H,3H-oxazolo[3,4-a]benzimidazoles: non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
Balzarini J
|
2001
|
Antiviral chemistry & chemotherapy
|
Rapid alternation of drug therapy is highly efficient in suppressing the emergence of mutant drug-resistant HIV strains in cell culture.
|
Balzarini J
|
2001
|
AIDS research and human retroviruses
|
Anti-HIV-1 activity of benzothiadiazine dioxide.
|
Balzarini J
|
2001
|
Antiviral chemistry & chemotherapy
|
Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.
|
Balzarini J
|
2001
|
Bioorganic & medicinal chemistry letters
|
Mutations at amino acid positions 63, 189, and 396 of human immunodeficiency virus type 1 reverse transcriptase (RT) partially restore the DNA polymerase activity of a Trp229Tyr mutant RT.
|
Balzarini J
|
2001
|
Virology
|
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
|
Balzarini J
|
2001
|
Journal of medicinal chemistry
|
Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.
|
Balzarini J
|
2001
|
Virology
|
Mutational analysis of trp-229 of human immunodeficiency virus type 1 reverse transcriptase (RT) identifies this amino acid residue as a prime target for the rational design of new non-nucleoside RT inhibitors.
|
Balzarini J
|
2000
|
Molecular pharmacology
|
Partial purification and characterization of mitochondrial DNA polymerase from Plasmodium falciparum.
|
Balzarini J
|
2000
|
Parasitol Int
|
Long-term exposure of HIV type 1-infected cell cultures to combinations of the novel quinoxaline GW420867X with lamivudine, abacavir, and a variety of nonnucleoside reverse transcriptase inhibitors.
|
Balzarini J
|
2000
|
AIDS research and human retroviruses
|
Phenylethylthiazolylthiourea (PETT) non-nucleoside inhibitors of HIV-1 and HIV-2 reverse transcriptases. Structural and biochemical analyses.
|
Balzarini J
|
2000
|
The Journal of biological chemistry
|
Anti-(herpes simplex virus) activity of 4'-thio-2'-deoxyuridines: a biochemical investigation for viral and cellular target enzymes.
|
Balzarini J
|
2000
|
The Biochemical journal
|
Evaluation of Compounds Against Recombinant HIV Reverse Transcriptase.
|
Balzarini J
|
2000
|
Methods in molecular medicine
|
Evaluating Clinical Isolates for Their Phenotypic and Genotypic Resistance Against Anti-HIV Drugs.
|
Balzarini J
|
2000
|
Methods in molecular medicine
|
Human immunodeficiency virus type 1 reverse transcriptase dimer destabilization by 1-[Spiro[4"-amino-2",2" -dioxo-1",2" -oxathiole-5",3'-[2', 5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]]]-3-ethylthy mine.
|
Balzarini J
|
2000
|
Biochemistry
|
Presence of 2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxath iole-2",2"-dioxide) (TSAO)-resistant virus strains in TSAO-inexperienced HIV patients.
|
Balzarini J
|
2000
|
AIDS research and human retroviruses
|
Suppression of resistance to drugs targeted to human immunodeficiency virus reverse transcriptase by combination therapy.
|
Balzarini J
|
1999
|
Biochemical pharmacology
|
Synthesis and anti-HIV activity of 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazines (TTDs): a new family of HIV-1 specific non-nucleoside reverse transcriptase inhibitors.
|
Balzarini J
|
1999
|
Bioorganic & medicinal chemistry
|
Potential multifunctional inhibitors of HIV-1 reverse transcriptase. Novel [AZT]-[TSAO-T] and [d4T]-[TSAO-T] heterodimers modified in the linker and in the dideoxynucleoside region.
|
Balzarini J
|
1999
|
Journal of medicinal chemistry
|
Role of antimetabolites of purine and pyrimidine nucleotide metabolism in tumor cell differentiation.
|
Balzarini J
|
1999
|
Biochemical pharmacology
|
9-(2-Phosphonylmethoxyethyl)adenine induces tumor cell differentiation or cell death by blocking cell cycle progression through the S phase.
|
Balzarini J
|
1999
|
Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research
|
A proline-to-histidine substitution at position 225 of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) sensitizes HIV-1 RT to BHAP U-90152.
|
Balzarini J
|
1998
|
The Journal of general virology
|
Crystal structures of HIV-1 reverse transcriptase in complex with carboxanilide derivatives.
|
Balzarini J
|
1998
|
Biochemistry
|
Treatment of visna virus infection in lambs with the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)adenine (PMEA).
|
Balzarini J
|
1998
|
Antiviral chemistry & chemotherapy
|
An approach towards the synthesis of potential metal-chelating TSAO-T derivatives as bidentate inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
|
Balzarini J
|
1998
|
Antiviral chemistry & chemotherapy
|
Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase.
|
Balzarini J
|
1998
|
Journal of medicinal chemistry
|
Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication.
|
Balzarini J
|
1998
|
Journal of medicinal chemistry
|
1,1,3-Trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine (TTD) derivatives: a new class of nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors with anti-HIV-1 activity.
|
Balzarini J
|
1998
|
Antimicrobial agents and chemotherapy
|
Zidovudine-resistant human immunodeficiency virus type 1 strains subcultured in the presence of both lamivudine and quinoxaline HBY 097 retain marked sensitivity to HBY 097 but not to lamivudine.
|
Balzarini J
|
1997
|
The Journal of infectious diseases
|
Varicella-zoster virus thymidine kinase gene and antiherpetic pyrimidine nucleoside analogues in a combined gene/chemotherapy treatment for cancer.
|
Balzarini J
|
1997
|
Gene therapy
|
Inhibition of replication of HIV in primary monocyte/macrophages by different antiviral drugs and comparative efficacy in lymphocytes.
|
Balzarini J
|
1997
|
Journal of leukocyte biology
|
Models which explain the inhibition of reverse transcriptase by HIV-1-specific (thio)carboxanilide derivatives.
|
Balzarini J
|
1997
|
Biochemical and biophysical research communications
|
SIV/HIV-1 hybrid virus expressing the reverse transcriptase gene of HIV-1 remains sensitive to HIV-1-specific reverse transcriptase inhibitors after passage in rhesus macaques.
|
Balzarini J
|
1997
|
Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association
|
SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus.
|
Balzarini J
|
1997
|
Antimicrobial agents and chemotherapy
|
Reverse transcriptase fidelity and HIV-1 variation.
|
Balzarini J
|
1997
|
Science (New York, N.Y.)
|
Characteristics of the Pro225His mutation in human immunodeficiency virus type 1 (HIV-1) reverse transcriptase that appears under selective pressure of dose-escalating quinoxaline treatment of HIV-1.
|
Balzarini J
|
1997
|
Journal of virology
|
Anti-HIV and anti-HBV activity and resistance profile of 2',3'-dideoxy-3'-thiacytidine (3TC) and its arylphosphoramidate derivative CF 1109.
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Balzarini J
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1996
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Biochemical and biophysical research communications
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Analysis of inhibition of retroviral reverse transcriptase.
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Balzarini J
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1996
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Methods in enzymology
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Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication.
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Balzarini J
|
1996
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Molecular pharmacology
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Marked inhibitory activity of non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus type 1 when combined with (-)2',3'-dideoxy-3'-thiacytidine.
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Balzarini J
|
1996
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Molecular pharmacology
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Identification of novel thiocarboxanilide derivatives that suppress a variety of drug-resistant mutant human immunodeficiency virus type 1 strains at a potency similar to that for wild-type virus.
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Balzarini J
|
1996
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Antimicrobial agents and chemotherapy
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Differences in the inhibition of human immunodeficiency virus type 1 reverse transcriptase DNA polymerase activity by analogs of nevirapine and [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1", 2"-oxathiole-2",2"-dioxide] (TSAO).
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Balzarini J
|
1996
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Molecular pharmacology
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Novel L-lyxo and 5'-deoxy-5'-modified TSAO-T analogs: synthesis and anti-HIV-1 activity.
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Balzarini J
|
1996
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Antiviral research
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A two plasmid co-expression system in Escherichia coli for the production of virion-like reverse transcriptase of the human immunodeficiency virus type 1.
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Balzarini J
|
1996
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Journal of virological methods
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Potent inhibition of human immunodeficiency virus and herpes simplex virus type 1 by 9-(2-phosphonylmethoxyethyl)adenine in primary macrophages is determined by drug metabolism, nucleotide pools, and cytokines.
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Balzarini J
|
1996
|
Molecular pharmacology
|
Cytotoxicity of 3'-azido-3'-deoxythymidine correlates with 3'-azidothymidine-5'-monophosphate (AZTMP) levels, whereas anti-human immunodeficiency virus (HIV) activity correlates with 3'-azidothymidine-5'-triphosphate (AZTTP) levels in cultured CEM T-lymphoblastoid cells.
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Balzarini J
|
1995
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Biochemical pharmacology
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Suppression of the breakthrough of human immunodeficiency virus type 1 (HIV-1) in cell culture by thiocarboxanilide derivatives when used individually or in combination with other HIV-1-specific inhibitors (i.e., TSAO derivatives).
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Balzarini J
|
1995
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Proceedings of the National Academy of Sciences of the United States of America
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Knocking out human immunodeficiency virus through non-nucleoside reverse transcriptase inhibitors used as single agents or in combinations: a paradigm for the cure of AIDS?
|
Balzarini J
|
1995
|
Farmaco (Società chimica italiana : 1989)
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Sensitivity/resistance profile of a simian immunodeficiency virus containing the reverse transcriptase gene of human immunodeficiency virus type 1 (HIV-1) toward the HIV-1-specific non-nucleoside reverse transcriptase inhibitors.
|
Balzarini J
|
1995
|
Biochemical and biophysical research communications
|
Activity of various thiocarboxanilide derivatives against wild-type and several mutant human immunodeficiency virus type 1 strains.
|
Balzarini J
|
1995
|
Antiviral research
|
Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase.
|
Balzarini J
|
1995
|
Journal of medicinal chemistry
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Differential activities of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives against different human immunodeficiency virus type 1 mutant strains.
|
Balzarini J
|
1995
|
Antimicrobial agents and chemotherapy
|
Novel concepts in the treatment of human immunodeficiency virus type 1 (HIV-1) infections by HIV-1-specific reverse transcriptase inhibitors.
|
Balzarini J
|
1995
|
Verhandelingen - Koninklijke Academie voor Geneeskunde van België
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Resistance pattern of human immunodeficiency virus type 1 reverse transcriptase to quinoxaline S-2720.
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Balzarini J
|
1994
|
Journal of virology
|
Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K)RT HIV-1 mutants or select for highly resistant (Y181C-->C181I)RT HIV-1 mutants.
|
Balzarini J
|
1994
|
Proceedings of the National Academy of Sciences of the United States of America
|
The synthesis of nucleoside 5'-O-(1,1-dithiotriphosphates).
|
Balzarini J
|
1994
|
Journal of medicinal chemistry
|
Resistance of HIV-1 reverse transcriptase against [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2''-dioxide)] (TSAO) derivatives is determined by the mutation Glu138-->Lys on the p51 subunit.
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Balzarini J
|
1994
|
The Journal of biological chemistry
|
Sensitivity of (138 Glu-->Lys) mutated human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) to HIV-1-specific RT inhibitors.
|
Balzarini J
|
1994
|
Biochemical and biophysical research communications
|
Comparative cytostatic activity of different antiherpetic drugs against herpes simplex virus thymidine kinase gene-transfected tumor cells.
|
Balzarini J
|
1994
|
Molecular pharmacology
|
Inhibition of visna virus replication by 2',3'-dideoxynucleosides and acyclic nucleoside phosphonate analogs.
|
Balzarini J
|
1993
|
Antimicrobial agents and chemotherapy
|
Knocking-out concentrations of HIV-1-specific inhibitors completely suppress HIV-1 infection and prevent the emergence of drug-resistant virus.
|
Balzarini J
|
1993
|
Virology
|
Human immunodeficiency virus type 1 (HIV-1) strains selected for resistance against the HIV-1-specific [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro- 5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)]-beta-D-pentofurano syl (TSAO) nucleoside analogues retain sensitivity to HIV-1-specific nonnucleoside inhibitors.
|
Balzarini J
|
1993
|
Proceedings of the National Academy of Sciences of the United States of America
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Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy.
|
Balzarini J
|
1993
|
Journal of virology
|
Human immunodeficiency virus type 1 drug-resistance patterns with different 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives.
|
Balzarini J
|
1993
|
Molecular pharmacology
|
HIV-1-specific reverse transcriptase inhibitors show differential activity against HIV-1 mutant strains containing different amino acid substitutions in the reverse transcriptase.
|
Balzarini J
|
1993
|
Virology
|
Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type 1-specific non-nucleoside analogues.
|
Balzarini J
|
1993
|
Molecular pharmacology
|
2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2'-dioxide)pyrimidine (TSAO) nucleoside analogues: highlyselective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase.
|
Balzarini J
|
1992
|
Proceedings of the National Academy of Sciences of the United States of America
|
[2',5'-Bis-O-(tert-butyldimethylsilyl)]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide) (TSAO) derivatives of purine and pyrimidinenucleosides as potent and selective inhibitors of human immunodeficiency virus type 1.
|
Balzarini J
|
1992
|
Antimicrobial agents and chemotherapy
|
Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents.
|
Balzarini J
|
1992
|
Molecular pharmacology
|
3'-C-branched 2'-deoxy-5-methyluridines: synthesis, enzyme inhibition, and antiviral properties.
|
Balzarini J
|
1992
|
Journal of medicinal chemistry
|
Anti-human immunodeficiency virus effects of cationic metalloporphyrin-ellipticine complexes.
|
Balzarini J
|
1992
|
Biochemical pharmacology
|
Selective inhibition of HIV replication by adriamycin in macrophages but not in lymphocytes.
|
Balzarini J
|
1992
|
AIDS research and human retroviruses
|
Kinetics of inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase by the novel HIV-1-specific nucleoside analogue [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5 "- (4"-amino-1",2"-oxathiole-2",2"-dioxide)thymine (TSAO-T).
|
Balzarini J
|
1992
|
The Journal of biological chemistry
|
Differential inhibition of retroviral reverse transcriptase by poly(2-fluoroadenylic acid), a template analogue.
|
Balzarini J
|
1991
|
AIDS (London, England)
|
5-Phosphoribosyl 1-pyrophosphate synthetase converts the acyclic nucleoside phosphonates 9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine and 9-(2-phosphonylmethoxyethyl)adenine directly to their antivirally active diphosphate derivatives.
|
Balzarini J
|
1991
|
The Journal of biological chemistry
|
9-[(2RS)-3-fluoro-2-phosphonylmethoxypropyl] derivatives of purines: a class of highly selective antiretroviral agents in vitro and in vivo.
|
Balzarini J
|
1991
|
Proceedings of the National Academy of Sciences of the United States of America
|
Intracellular metabolism and mechanism of anti-retrovirus action of 9-(2-phosphonylmethoxyethyl)adenine, a potent anti-human immunodeficiency virus compound.
|
Balzarini J
|
1991
|
Proceedings of the National Academy of Sciences of the United States of America
|
Potent DNA chain termination activity and selective inhibition of human immunodeficiency virus reverse transcriptase by 2',3'-dideoxyuridine-5'-triphosphate.
|
Balzarini J
|
1990
|
Molecular pharmacology
|
Differential inhibitory effects of several pyrimidine 2',3'-dideoxynucleoside 5'-triphosphates on the activities of reverse transcriptase and various cellular DNA polymerases.
|
Balzarini J
|
1989
|
Molecular pharmacology
|
Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative.
|
Balzarini J
|
1989
|
Biochemical and biophysical research communications
|
Differential inhibition of various deoxyribonucleic acid polymerases by Evans blue and aurintricarboxylic acid.
|
Balzarini J
|
1988
|
European journal of biochemistry / FEBS
|
Fuchsin acid selectively inhibits human immunodeficiency virus (HIV) replication in vitro.
|
Balzarini J
|
1988
|
Biochemical and biophysical research communications
|
Mechanism of inhibitory effect of dextran sulfate and heparin on replication of human immunodeficiency virus in vitro.
|
Balzarini J
|
1988
|
Proceedings of the National Academy of Sciences of the United States of America
|
Alpha, beta- and beta, gamma-methylene 5'-phosphonate derivatives of 3'-azido-2',3'-dideoxythymidine-5'-triphosphate. Correlation between affinity for reverse transcriptase, susceptibility to hydrolysis by phosphodiesterases and anti-retrovirus activity.
|
Balzarini J
|
1988
|
Biochemical pharmacology
|
Comparative inhibitory effects of suramin and other selected compounds on the infectivity and replication of human T-cell lymphotropic virus (HTLV-III)/lymphadenopathy-associated virus (LAV).
|
Balzarini J
|
1986
|
International journal of cancer. Journal international du cancer
|
Aurintricarboxylic acid and Evans Blue represent two different classes of anionic compounds which selectively inhibit the cytopathogenicity of human T-cell lymphotropic virus type III/lymphadenopathy-associated virus.
|
Balzarini J
|
1986
|
Biochemical and biophysical research communications
|
Antiviral activity of the 3'-amino derivative of (E)-5-(2-bromovinyl)-2'-deoxyuridine.
|
Balzarini J
|
1983
|
The Biochemical journal
|