Discovery of Mcl-1 inhibitors based on a thiazolidine-2,4-dione scaffold
2017
Abstarct Inspired by a rhodanine-based dual inhibitor of Bcl-x L and Mcl-1, a focused library of analogues was prepared wherein the rhodanine core was replaced with a less promiscuous thiazolidine-2,4-dione scaffold. Compounds were initially evaluated for their abilities to inhibit Mcl-1. The most potent compound 12b inhibited Mcl-1 with a K i of 155 nM. Further investigation revealed comparable inhibition of Bcl-x L ( K i = 90 nM), indicating that the dual inhibitory profile of the initial rhodanine lead had been retained upon switching the heterocycle core.
Keywords:
- Correction
- Source
- Cite
- Save
- Machine Reading By IdeaReader
21
References
8
Citations
NaN
KQI