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- W2772473038 abstract "Inspired by a rhodanine-based dual inhibitor of Bcl-xL 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 Ki of 155 nM. Further investigation revealed comparable inhibition of Bcl-xL (Ki = 90 nM), indicating that the dual inhibitory profile of the initial rhodanine lead had been retained upon switching the heterocycle core." @default.
- W2772473038 created "2017-12-22" @default.
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- W2772473038 date "2018-02-01" @default.
- W2772473038 modified "2023-09-27" @default.
- W2772473038 title "Discovery of Mcl-1 inhibitors based on a thiazolidine-2,4-dione scaffold" @default.
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- W2772473038 doi "https://doi.org/10.1016/j.bmcl.2017.11.023" @default.
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