期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 11, 页码 3839-3853出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm200148p
关键词
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资金
- NIH/NCI [CA120458]
- ACS Division of Organic Chemistry
Development of the DNA gyrase inhibitor, novobiocin, into a selective Hsp90 inhibitor was accomplished through structural modifications to the amide side chain, coumarin ring, and sugar moiety. These species exhibit similar to 700-fold improved anti-proliferative activity versus the natural product as evaluated by cellular efficacies against breast, colon, prostate, lung, and other cancer cell lines. Utilization of structure-activity relationships established for three novobiocin synthons produced optimized scaffolds, which manifest midnanomolar activity against a panel of cancer cell lines and serve as lead compounds that manifest their activities through Hsp90 inhibition.
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