Article
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
Journal of medicinal chemistry - 11 Feb 2010
Xue Hai, Lu Xiaofan, Zheng Purong, Liu Li, Han Chunyan, Hu Jinping, Liu Zijie, Ma Tao, Li Yan, Wang Lin, Chen Zhiwei, Liu Gang
Abstract excerpt
We herein report a new compound: 10-chloromethyl-11-demethyl-12-oxo-calanolide A (20, EC(50) = 7.4 nM, SI = 1417), which demonstrates a druggable profile with 32.7% oral bioavailability in rat, tolerated oral single dose toxicity in mice, and especially the feature of highly efficient suppression...
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