Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 53, Issue 3, Pages 1397-1401Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm901653e
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Funding
- National Natural Science Foundation of China [90713045]
- National 863 Program of China [2006AA020501]
- HKU-UDF
- HKSARG [FHB/RFCID09080772]
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We herein report a new compound: 10-chloromethyl-11-demethyl-12-oxo-calanolide A (20, EC50 = 7.4 nM, St = 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.
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