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
2008
发表期刊CHEMISTRY & BIODIVERSITY
卷号5期号:3页码:447-460
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.
关键词Cyclohexapeptide Annomuricatin a
收录类别SCI
语种英语
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
WOS类目Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary
WOS记录号WOS:000254845900009
引用统计
被引频次:34[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/4016
专题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
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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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