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合成及穿心莲内酯衍生物的初步抗 HIV 活性。

Synthesis and preliminary anti-HIV activities of andrographolide derivatives.

机构信息

Center of Drug Discovery, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.

出版信息

Med Chem. 2010 Jul;6(4):252-8. doi: 10.2174/1573406411006040252.

DOI:10.2174/1573406411006040252
PMID:20879977
Abstract

Recent studies indicated that andrographolide was a potential anti-HIV therapeutic agent. In the paper, the synthesis of a series of andrographolide derivatives was described and their anti-HIV activities were evaluated in vitro. As compared with TI, compounds 5c, 5d and 5i showed moderate inhibitory activities on the cytopathic effect with TI above 10. Among the derivatives, compound 5i was the best one with TI > 51.

摘要

最近的研究表明,穿心莲内酯是一种有潜力的抗 HIV 治疗药物。本文描述了一系列穿心莲内酯衍生物的合成,并对它们的体外抗 HIV 活性进行了评价。与 TI 相比,化合物 5c、5d 和 5i 对细胞病变效应的抑制活性中等,TI 值均大于 10。在这些衍生物中,化合物 5i 的 TI 值最大,超过 51。

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