Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors
文献类型：期刊论文
| 作者 | Ma XD1; He QQ1; Zhang X2,3; Yang SQ1; Yang LM2; Gu SX1; Zheng YT2; Chen FE[*]1,4; Dai HF[*]5 |
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012 |
| 卷号 | 58期号:X页码:504-512 |
| 关键词 | Anti-HIV activity NNRTIs Benzophenone derivatives N-Phenylarylformamide Structure-activity relationship |
| 通讯作者 | rfchen@fudan.edu.cn |
| 合作状况 | 其它 |
| 英文摘要 | A series of N-phenylarylformamide derivatives (PAFAs) with anti-wild-type HIV-1 activity (EC50 values) ranging from 0.3 nM to 5.1 nM and therapeutic index (TI) ranging from 10 616 to 271 000 were identified as novel non-nucleoside reverse transcriptase inhibitors. Among them, compound 13g (EC50 = 0.30 nM, TI = 184 578), 131 (EC50 = 0.37 nM, TI = 212 819), 13m (EC50 = 0.32 nM, TI = 260 617) and 13r (EC50 = 0.27 nM, TI = 271 000) displayed the highest activity against this type virus nearly as potent as lead compound GW678248. Moreover, all of them were also active to inhibit the double mutant strain A(17) (K103N + Y181C) with EC50 values of 0.29 mu M, 0.14 mu M, 0.10 mu M and 0.27 mu M, respectively. In particular, compound 13m, which showed broad-spectrum anti-HIV activity, was also effective to inhibit the HIV-2 ROD replication within 4.37 mu M concentration. (C) 2012 Elsevier Masson SAS. All rights reserved. |
| 收录类别 | SCI |
| 资助信息 | This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029). |
| 语种 | 英语 |
| WOS记录号 | WOS:000312745100053 |
| 公开日期 | 2013-03-08 |
| 源URL | [http://159.226.149.42:8088/handle/152453/7271]  |
| 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.Department of Chemistry, Fudan University, Shanghai 200433, PR China 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 650223, PR China 3.Graduate School of the Chinese Academy of Sciences, Beijing 100039, PR China 4.Institute of Biomedical Science, Fudan University, Shanghai 200031, PR China 5.School of Pharmacy, Fudan University, Shanghai 200031, PR China |
| 推荐引用方式 GB/T 7714 | Ma XD,He QQ,Zhang X,et al. Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,58(X):504-512. |
| APA | Ma XD.,He QQ.,Zhang X.,Yang SQ.,Yang LM.,...&Dai HF[*].(2012).Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,58(X),504-512. |
| MLA | Ma XD,et al."Synthesis, structure-activity relationships, and docking studies of N-phenylarylformamide derivatives (PAFAs) as non-nucleoside HIV reverse transcriptase inhibitors".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 58.X(2012):504-512. |
入库方式： OAI收割
来源：昆明动物研究所
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