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Highly Suppressing Wild-Type HIV-1 and Y181C Mutant HIV-1 Strains by 10-Chloromethyl-11-demethyl-12-oxo-calanolide A with Druggable Profile

2010; American Chemical Society; Volume: 53; Issue: 3 Linguagem: Inglês

10.1021/jm901653e

1520-4804

Hai Xue, Xiaofan Lu, Purong Zheng, Li Liu, Chunyan Han, Jinping Hu, Zijie Liu, Tao Ma, Yan Li, Lin Wang, Zhiwei Chen, Gang Liu,

Hepatitis C virus research

We herein report a new compound: 10-chloromethyl-11-demethyl-12-oxo-calanolide A (20, EC50 = 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 of the wild-type HIV-1 and Y181C mutant HIV-1 at an EC50 = 7.4 nM and EC50 = 0.46 nM, respectively.