Synthesis of analogues of flazin, in particular, flazinamide, as promising Anti-HIV agents | |
Tang, Jian-Guo2,3; Wang, Yun-Hua1,3; Wang, Rui-Rui1,3; Dong, Ze-Jun2; Yang, Liu-Meng1; Zheng, Yong-Tang1; Liu, Ji-Kai2 | |
刊名 | CHEMISTRY & BIODIVERSITY |
2008 | |
卷号 | 5期号:3页码:447-460 |
关键词 | Cyclohexapeptide Annomuricatin a |
文献子类 | Article |
英文摘要 | Flazin isolated from the fruiting bodies of Suillus granulatus was found to possess weak anti-HIV activity (EC50=2.36 mu m, TI= 12.1). To establish a SAR study, 46 flazin analogues were synthesized, and their anti-HIV activities were evaluated in vitro. Among them, flazinamide (9a) showed the most potent activity with an EC50 value of 0.38 pm and a TI value of 312.0. The results suggested that appropriate substituents at positions 3, 1', and 5' of flazin might play a crucial role in determining their anti-HIV activities, and that flazinamide can be considered as a promising, readily available anti-HIV agent. |
WOS关键词 | INDOLYL ARYL SULFONES ; BENZODIAZEPINE RECEPTOR ; REVERSE-TRANSCRIPTASE ; DERIVATIVES ; INHIBITOR ; DESIGN ; RESISTANCE ; ACID |
WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
语种 | 英语 |
WOS记录号 | WOS:000254845900009 |
公开日期 | 2012-03-21 |
内容类型 | 期刊论文 |
源URL | [http://ir.kib.ac.cn:8080/handle/151853/4016] |
专题 | 昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室 |
作者单位 | 1.Chinese Acad Sci, Kunming Inst Zool, Key Lab Anim Models & Human Dis Mech, Lab Mol Immunopharmacol, Kunming 650223, Peoples R China 2.Chinese Acad Sci, Kunming Inst Zool, State Key Lab Phytochem & Plant Resources W China, Kunming 650223, Peoples R China 3.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China |
推荐引用方式 GB/T 7714 | Tang, Jian-Guo,Wang, Yun-Hua,Wang, Rui-Rui,et al. Synthesis of analogues of flazin, in particular, flazinamide, as promising Anti-HIV agents[J]. CHEMISTRY & BIODIVERSITY,2008,5(3):447-460. |
APA | Tang, Jian-Guo.,Wang, Yun-Hua.,Wang, Rui-Rui.,Dong, Ze-Jun.,Yang, Liu-Meng.,...&Liu, Ji-Kai.(2008).Synthesis of analogues of flazin, in particular, flazinamide, as promising Anti-HIV agents.CHEMISTRY & BIODIVERSITY,5(3),447-460. |
MLA | Tang, Jian-Guo,et al."Synthesis of analogues of flazin, in particular, flazinamide, as promising Anti-HIV agents".CHEMISTRY & BIODIVERSITY 5.3(2008):447-460. |
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