Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
文献类型：期刊论文
| 作者 | Ma XD1; Zhang X4,5; Yang SQ1; Dai HF3; 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:16页码:4704-4709 |
| 关键词 | HIV NNRTIs Benzophenone derivatives Benzhydrol SAR |
| 通讯作者 | rfchen@fudan.edu.cn |
| 合作状况 | 其它 |
| 英文摘要 | A series of (+/-)-benzhydrol derivatives featuring the essential sulfonamide group at the para position on the C-ring were synthesized and evaluated for the potential anti-HIV activity in C8166 cells. Most of these analogues demonstrated low concentration inhibitory activity with EC(50) values less than 1 mu M against the wild-type HIV-1. In particular, compound 7h was identified as the highest active inhibitor of wildtype HIV-1 with an EC(50) value of 0.12 mu M and selectivity index value of 312.73. Furthermore, some of them also exhibited moderate activity against the double mutant strain A(17) (K103N + Y181C) with EC(50) values lower than 5 mu M. In addition, the binding modes with RT and the preliminary structure-activity relationships of these derivatives were also explored for further chemical modifications. |
| 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 | 2011-08-26 |
| 源URL | [http://159.226.149.42:8088/handle/353002/6712]  |
| 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.Graduate School of the Chinese Academy of Sciences, Beijing 100039, PR China |
| 推荐引用方式 GB/T 7714 | Ma XD,Zhang X,Yang SQ,et al. Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2011,19(16):4704-4709. |
| APA | Ma XD.,Zhang X.,Yang SQ.,Dai HF.,Yang LM.,...&Chen FE[*].(2011).Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.BIOORGANIC & MEDICINAL CHEMISTRY,19(16),4704-4709. |
| MLA | Ma XD,et al."Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors".BIOORGANIC & MEDICINAL CHEMISTRY 19.16(2011):4704-4709. |
入库方式： OAI收割
来源：昆明动物研究所
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