Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors
文献类型：期刊论文
| 作者 | Sun YM1; Lu CL2,3; Wang CY1; Wang RR2; Liu KX1; Yang LM2; Zhen YH1; Zhang HL1; Wang C1; Zheng YT[*]2 |
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2015 |
| 卷号 | 26期号:2页码:243-247 |
| 关键词 | Benzophenone N-Phenylbenzenesulfonamide Structure modification Anti-HIV activity |
| 通讯作者 | zhengyt@mail.kiz.ac.cn ; xiaodong.ma@139.com |
| 合作状况 | 其它 |
| 英文摘要 | Searching for more safe and effective agents for HIV treatments is still an urgent topic worldwide. Based on our continuous modifications on the benzophenone derivatives as HIV-1 reverse transcriptase (RT) inhibitors, a new template bearing N-phenylbenzenesulfonamide (PBSA) structure was designed to enhance the interactions with HIV-1 RT. In this manuscript, a series of PBSA derivatives were synthesized and evaluated for their anti-HIV-1 activity. The preliminary test showed that these compounds were potent to inhibit wild-type HIV-1 with EC50 values ranging of 0.105-14.531 mu mol/L. In particular, compound 13f not only has high anti-HIV-1 activity (0.108 mu mol/L), but also possesses low toxicity with a TI value of 1816.6. Furthermore, the major interactions of the inhibitor 13f with HIV-1 RT were also investigated using the molecular modelling. Our discovered structure-activity relationships (SARs) of these analogues may serve as an important clue for further optimizations. |
| 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 (No. 81402788), and the Ph.D. Start-up Fund of Natural Science Foundation of Liaoning Province, China (No. 20141115). |
| 语种 | 英语 |
| WOS记录号 | WOS:000351649200017 |
| 公开日期 | 2015-04-24 |
| 源URL | [http://159.226.149.42:8088/handle/152453/8314]  |
| 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.College of Pharmacy, Dalian Medical University, Dalian 116044, China 2.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China 3.Kunming College of Life Science, University of Chinese Academy of Sciences, Kunming 650204, China |
| 推荐引用方式 GB/T 7714 | Sun YM,Lu CL,Wang CY,et al. Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors[J]. CHINESE CHEMICAL LETTERS,2015,26(2):243-247. |
| APA | Sun YM.,Lu CL.,Wang CY.,Wang RR.,Liu KX.,...&Ma XD[*].(2015).Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors.CHINESE CHEMICAL LETTERS,26(2),243-247. |
| MLA | Sun YM,et al."Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors".CHINESE CHEMICAL LETTERS 26.2(2015):243-247. |
入库方式： OAI收割
来源：昆明动物研究所
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