Article
Structure-activity relationship studies of phenanthridine-based Bcl-XL inhibitors.
Journal of medicinal chemistry - 13 Nov 2008
Bernardo Paul H, Wan Kah-Fei, Sivaraman Thirunavukkarasu, Xu Jin, Moore Felicity K, Hung Alvin W, Mok Henry Y K, Yu Victor C, Chai Christina L L
Abstract excerpt
Despite their structural similarities, the natural products chelerythrine ( 5) and sanguinarine ( 6) target different binding sites on the pro-survival Bcl-X L protein. This paper details the synthesis of phenanthridine-based analogues of the natural products that were used to probe this difference in binding profiles. The inhibitory constants for these compounds were then measured in a fluorescence polarization...
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