Effect of human serum on the in vitro anti-HIV-1 activity of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) derivatives as related to their lipophilicity and serum protein binding.

[1]  R T Walker,et al.  Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) as potent and selective anti-HIV-1 agents. , 1992, Journal of medicinal chemistry.

[2]  E. De Clercq,et al.  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). , 1992, The Journal of biological chemistry.

[3]  E. De Clercq,et al.  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. , 1992, Proceedings of the National Academy of Sciences of the United States of America.

[4]  W. Schleif,et al.  L-696,229 specifically inhibits human immunodeficiency virus type 1 reverse transcriptase and possesses antiviral activity in vitro , 1992, Antimicrobial Agents and Chemotherapy.

[5]  E. De Clercq,et al.  Common features in the interaction of tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives with the human immunodeficiency virus type 1 reverse transcriptase. , 1992, Molecular pharmacology.

[6]  R. T. Walker,et al.  Highly potent and selective inhibition of HIV-1 replication by 6-phenylthiouracil derivatives. , 1992, Antiviral research.

[7]  Cheng Yung-Chi,et al.  HIV-1 reverse transcriptase inhibition by a dipyridodiazepinone derivative: BI-RG-587. , 1992 .

[8]  R T Walker,et al.  Structure-activity relationships of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine analogues: effect of substitutions at the C-6 phenyl ring and at the C-5 position on anti-HIV-1 activity. , 1992, Journal of medicinal chemistry.

[9]  R. Pauwels,et al.  A TIBO derivative, R82913, is a potent inhibitor of HIV-1 reverse transcriptase with heteropolymer templates. , 1991, Antiviral research.

[10]  L. Resnick,et al.  Nonnucleoside reverse transcriptase inhibitors that potently and specifically block human immunodeficiency virus type 1 replication. , 1991, Proceedings of the National Academy of Sciences of the United States of America.

[11]  K. Frank,et al.  Kinetic interaction of human immunodeficiency virus type 1 reverse transcriptase with the antiviral tetrahydroimidazo[4,5,1-jk]-[1,4]-benzodiazepine-2-(1H)-thione compound, R82150. , 1991, The Journal of biological chemistry.

[12]  W. Schleif,et al.  Pyridinone derivatives: specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity. , 1991, Proceedings of the National Academy of Sciences of the United States of America.

[13]  R. T. Walker,et al.  Highly potent and selective inhibition of human immunodeficiency virus type 1 by a novel series of 6-substituted acyclouridine derivatives. , 1991, Molecular pharmacology.

[14]  R T Walker,et al.  Synthesis and anti-HIV activity of 2-, 3-, and 4-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). , 1991, Journal of medicinal chemistry.

[15]  E. De Clercq,et al.  Potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) by 5-ethyl-6-phenylthiouracil derivatives through their interaction with the HIV-1 reverse transcriptase. , 1991, Proceedings of the National Academy of Sciences of the United States of America.

[16]  J. Proudfoot,et al.  A novel dipyridodiazepinone inhibitor of HIV-1 reverse transcriptase acts through a nonsubstrate binding site. , 1991, Biochemistry.

[17]  E. De Clercq,et al.  An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk] [1,4]benzodiazepin-2 (1H)-one and -thione derivatives. , 1991, Proceedings of the National Academy of Sciences of the United States of America.

[18]  S Shigeta,et al.  A new class of HIV-1-specific 6-substituted acyclouridine derivatives: synthesis and anti-HIV-1 activity of 5- or 6-substituted analogues of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT). , 1991, Journal of medicinal chemistry.

[19]  J. Adams,et al.  Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. , 1990, Science.

[20]  H. Mitsuya,et al.  Lipophilic halogenated congeners of 2',3'-dideoxypurine nucleosides active against human immunodeficiency virus in vitro. , 1990, Proceedings of the National Academy of Sciences of the United States of America.

[21]  Erik De Clercq,et al.  Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives , 1990, Nature.

[22]  R T Walker,et al.  Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative. , 1989, Biochemical and biophysical research communications.

[23]  R T Walker,et al.  A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. , 1989, Journal of medicinal chemistry.

[24]  E. De Clercq,et al.  5-Halogeno-3'-fluoro-2',3'-dideoxyuridines as inhibitors of human immunodeficiency virus (HIV): potent and selective anti-HIV activity of 3'-fluoro-2',3'-dideoxy-5-chlorouridine. , 1989, Molecular pharmacology.

[25]  E. De Clercq,et al.  Estimation of the lipophilicity of anti-HIV nucleoside analogues by determination of the partition coefficient and retention time on a Lichrospher 60 RP-8 HPLC column. , 1989, Biochemical and biophysical research communications.

[26]  J Desmyter,et al.  Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds. , 1988, Journal of virological methods.

[27]  N. Yamamoto,et al.  Infection of HTLV-III/LAV in HTLV-I-carrying cells MT-2 and MT-4 and application in a plaque assay. , 1985, Science.

[28]  J. Mccall Liquid-lipquid partition coefficients by high-pressure liquid chromatography. , 1975, Journal of medicinal chemistry.