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Hai-Qiu Wu Zi-Hong Yan Wen-Xue Chen Qiu-Qin He Fen-Er Chen Erik De Clercq Jan Balzarini Dirk Daelemans Christophe Pannecouque 《Bioorganic & medicinal chemistry》2013,21(21):6477-6483
A series of C6-rigid S-DABO analogs characterized by a substituted benzoyl group at C6 position of the pyrimidine ring has been synthesized and biological evaluation as NNRTIs against wild-type HIV-1 strain IIIB, double RT mutant (K103N + Y181C) strain RES056 as well as HIV-2 strain ROD in MT-4 cell cultures. Most of the compounds exhibited moderate antiviral activities. Among them, compound 7q displayed the highest anti-HIV-1 activity with an EC50 value of 0.26 μM and a selectivity index (SI) of 541. The preliminary structure–activity relationship (SAR) of these new S-DABOs was investigated, the target RT was confirmed and docking study was performed. 相似文献
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《Bioorganic & medicinal chemistry》2014,22(4):1459-1467
A series of novel N1-aryl-2-arylthioacetamido-benzimidazoles were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Some of them proved to be effective in inhibiting HIV-1 replication at submicromolar and nanomolar concentration acting as HIV-1 non-nucleoside RT inhibitors (NNRTIs), with low cytotoxicity. The preliminary structure–activity relationship (SAR) of these new derivatives was discussed and rationalized by docking studies. 相似文献
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《Bioorganic & medicinal chemistry》2019,27(17):3836-3845
A novel series of 3-hydroxyquinazoline-2,4(1H,3H)-diones derivatives has been designed and synthesized. Their biochemical characterization revealed that most of the compounds were effective inhibitors of HIV-1 RNase H activity at sub to low micromolar concentrations. Among them, II-4 was the most potent in enzymatic assays, showing an IC50 value of 0.41 ± 0.13 μM, almost five times lower than the IC50 obtained with β-thujaplicinol. In addition, II-4 was also effective in inhibiting HIV-1 IN strand transfer activity (IC50 = 0.85 ± 0.18 μM) but less potent than raltegravir (IC50 = 71 ± 14 nM). Despite its relatively low cytotoxicity, the efficiency of II-4 in cell culture was limited by its poor membrane permeability. Nevertheless, structure-activity relationships and molecular modeling studies confirmed the importance of tested 3-hydroxyquinazoline-2,4(1H,3H)-diones as useful leads for further optimization. 相似文献
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Human immunodeficiency virus type-1 reverse transcriptase and ribonuclease h as substrates of the viral protease 下载免费PDF全文
Alfredo G. Tomasselli Jean L. Sarcich Linda J. Barrett Ilene M. Reardon W. Jeffrey Howe David B. Evans Satish K. Sharma Robert L. Heinrikson 《Protein science : a publication of the Protein Society》1993,2(12):2167-2176