Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents
文献类型：期刊论文
| 作者 | Ashok P1; Lu CL2,3; Chander S1; Zheng YT[*]2; Murugesan S[*]1 |
| 刊名 | CHEMICAL BIOLOGY & DRUG DESIGN
 |
| 出版日期 | 2015 |
| 卷号 | 85期号:6页码:722-728 |
| 关键词 | AIDS C8166 cells HAART HIV-1 indole p24 antigen beta-carboline |
| 通讯作者 | zhengyt@mail.kiz.ac.cn ; murugesan@pilani.bits-pilani.ac.in |
| 合作状况 | 其它 |
| 英文摘要 | 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. |
| 收录类别 | SCI |
| 公开日期 | 2015-06-08 |
| 源URL | [http://159.226.149.42:8088/handle/152453/8347]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 |
| 作者单位 | 1.Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Rajasthan 333031, India 2.Key laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China 3.Kunming College of Life Science, University of Chinese Academy of Sciences, Kunming, Yunnan 650204, China 4.Univ Chinese Acad Sci, Kunming Coll Life Sci, Kunming 650204, Yunnan, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ashok P,Lu CL,Chander S,et al. Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2015,85(6):722-728. |
| APA | Ashok P,Lu CL,Chander S,Zheng YT[*],&Murugesan S[*].(2015).Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents.CHEMICAL BIOLOGY & DRUG DESIGN,85(6),722-728. |
| MLA | Ashok P,et al."Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents".CHEMICAL BIOLOGY & DRUG DESIGN 85.6(2015):722-728. |
入库方式： OAI收割
来源：昆明动物研究所
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