科研成果
获奖成果
论文
专著
专利
现在位置:首页 > 科研成果 > 论文
论文
论文编号:
论文题目: Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents
作者: Penta Ashok; Cui-Lin Lu; Subhash Chander; Yong-Tang Zheng*; Sankarnarayanan Murugesan*
联系作者: zhengyt@mail.kiz.ac.cn; murugesan@pilani.bits-pilani.ac.in
外单位作者单位:
发表年度: 2015
卷: 85
期: 6
页码: 722-728
摘要: A novel series of 1-(thiophen-2-yl)-9H-pyrido [3,4-b]indole derivatives were synthesized using DL-tryptophan as starting material. All the compounds were characterized by spectral analysis such as H-1 NMR, Mass, IR, elemental analysis and evaluated for inhibitory potency against HIV-1 replication. Among the reported analogues, compound 7g exhibited significant anti-HIV activity with EC50 0.53m and selectivity index 483; compounds 7e, 7i, and 7o displayed moderate activity with EC50 3.8, 3.8, and 2.8m and selectivity index >105, >105, and 3.85, respectively. Interestingly, compound 7g inhibited p24 antigen expression in acute HIV-1(IIIB) infected cell line C8166 with EC50 1.1m. In this study, we also reported the Lipinski rule of 5 parameters, predicted toxicity profile, drug-likeness, and drug score of the synthesized analogues.
刊物名称: Chemical Biology & Drug Design
论文全文: 点击查看
全文链接: 点击下载
Email::
学科:
影响因子: 2.485 (2014)
第一作者所在部门:
论文出处:
论文类别:
参与作者: