Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors
文献类型：期刊论文
| 作者 | Ma XD1; Zhang X4,5; Dai HF3; Yang SQ1; Yang LM4; Gu SX1; Zheng YT4; He QQ1; Chen FE[*]1,2 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2011 |
| 卷号 | 19期号:15页码:4601-4607 |
| 关键词 | HIV NNRTIs Benzophenone derivatives Naphthyl SAR |
| 通讯作者 | rfchen@fudan.edu.cn |
| 合作状况 | 其它 |
| 英文摘要 | A novel series of benzophenone derivatives with B-ring substituted by naphthyl ring has been synthesized and evaluated as non-nucleoside HIV-1 reverse transcriptase inhibitors. Most of these compounds showed good to moderate activity against wild-type HIV-1 and mutated viruses. In particular, the analogue 10i demonstrated the most potent activity against wild-type HIV-1 with an EC(50) value of 4.8 nM, and with a high selectivity index up to 10347.9, it also proved to be active against the HIV-1 double mutant strain A(17) (K103N+Y181C) with an EC(50) value of 2.1 mu M. In addition, the molecular modeling study was used to explore the major interactions between the potent inhibitors with the HIV-1 RT. The investigation of the structure-activity relationships may serve as an important lead for the further optimization. |
| 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 |
| 公开日期 | 2011-08-09 |
| 源URL | [http://159.226.149.42:8088/handle/353002/6629]  |
| 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.Institute of Biomedical Science, Fudan University, Shanghai 200433, PR China 3.School of Pharmacy, Fudan University, Shanghai 200031, PR China 4.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 5.Faculty of Pharmacy, Kunming Medical University, Kunming 650031, PR China |
| 推荐引用方式 GB/T 7714 | Ma XD,Zhang X,Dai HF,et al. Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(15):4601-4607. |
| APA | Ma XD.,Zhang X.,Dai HF.,Yang SQ.,Yang LM.,...&Chen FE[*].(2011).Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,19(15),4601-4607. |
| MLA | Ma XD,et al."Synthesis and biological activity of naphthyl-substituted (B-ring) benzophenone derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 19.15(2011):4601-4607. |
入库方式： OAI收割
来源：昆明动物研究所
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