Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 11, Pages 3684-3687Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm048995+
Keywords
-
Categories
Ask authors/readers for more resources
Salinosporamide A (1, NPI-0052) is a potent proteasome inhibitor in development for treating cancer. In this study, a series of analogues was assayed for cytotoxicity, proteasome inhibition, and inhibition of NF-kappa B activation. Marked reductions in potency in cell-based assays accompanied replacement of the chloroethyl group with unhalogenated substituents. Halogen exchange and cyclohexene ring epoxidation were well tolerated, while some stereochemical modifications significantly attenuated activity. These findings provide insights into structure-activity relationships within this novel series.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available