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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: |
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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 |
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学科: |
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影响因子: |
2.485 (2014) |
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