新型非核苷类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

摘要: DCK是以天然产物为先导化合物经结构修饰得到的一个高活性抗HIV化合物，其作用机制独特，不同于现有的非核苷类逆转录酶抑制剂，高效低毒，有可能发展成为一类新的抗HIV药物。近年来以它为先导化合物进行了多方面的结构修饰，以期得到药用性质更好的化合物。本文就DCK的发现、结构修饰、构效关系及最新进展予以介绍。

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.