新型非核苷类抗HIV逆转录酶抑制剂DCK的研究进展

[Progress in the new nonnucleoside anti-HIV reverse transcriptase inhibitor-DCK].

作者信息

Guo Huan-fang, Xie Lan

机构信息

Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.

出版信息

Yao Xue Xue Bao. 2008 Oct;43(10):997-1002.

Abstract

3',4'-Di-O-(S)-comphanoyl-(+)-cis-khellactone (DCK) is a synthetic khellactone ester that exhibits potent anti-HIV activity with a mechanism distinct from clinically used anti-HIV agents. Several series of DCK analoges have been synthesized and evaluated for inhibitory effects against HIV. This review article describes recent progress in the discovery, structural modification, and structure-activity relationship studies of potent anti-HIV DCK derivatives.

摘要

3',4'-二-O-(S)-松柏酰基-(+)-顺式凯林内酯（DCK）是一种合成的凯林内酯酯，具有强大的抗HIV活性，其作用机制与临床使用的抗HIV药物不同。已经合成了几个系列的DCK类似物，并评估了它们对HIV的抑制作用。这篇综述文章描述了强效抗HIV DCK衍生物在发现、结构修饰和构效关系研究方面的最新进展。

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