Development and preclinical studies of broad-spectrum anti-HIV agent (3′ R, 4′ R)-3-cyanomethyl-4-methyl-3′, 4′-di-O-(S)-camphanoyl-(+)-cis-khellactone (3- …

…, XM Zhuang, AM Zhang, G Wu, JX Ruan…

Index: Xie, Lan; Guo, Huan-Fang; Lu, Hong; Zhuang, Xiao-Mei; Zhang, An-Ming; Wu, Gang; Ruan, Jin-Xiu; Zhou, Ting; Yu, Donglei; Qian, Keduo; Lee, Kuo-Hsiung; Jiang, Shibo Journal of Medicinal Chemistry, 2008 , vol. 51, # 24 p. 7689 - 7696

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Citation Number: 15

Abstract

In prior investigation, we discovered that (3′ R, 4′ R)-3-cyanomethyl-4-methyl-3′, 4′-di- O-(S)-camphanoyl-(+)-cis-khellactone (4, 3-cyanomethyl-4-methyl-DCK) showed promising anti-HIV activity. In these current studies, we developed and optimized successfully a practical 10-step synthesis for scale-up preparation to increase the overall yield of 4 from 7.8% to 32%. Furthermore, compound 4 exhibited broad-spectrum anti-HIV activity against ...