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- W3104394761 abstract "Abstract Pin1 is a peptidyl prolyl cis-trans isomerase (PPIase) and inhibiting Pin1 is a potential way for discovering anti-tumor agents. With an aim to find potent Pin1 inhibitors with a novel scaffold, a series of thiazole derivatives with an alicyclic heterocycles on the 2-position were designed, synthesized and tested against human Pin1. Compound 9p bearing a 2-oxa-6-azaspiro [3,3] heptane moiety on the thiazole scaffold was identified as the most potent Pin1 inhibitor of this series with an IC50 value of 0.95 μM. The structure-activity relationship (SAR) and molecular modeling study indicated that introducing an alicyclic ring with an H-bond acceptor would be a viable way to improve the binding affinity." @default.
- W3104394761 created "2020-11-23" @default.
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- W3104394761 date "2021-01-01" @default.
- W3104394761 modified "2023-10-03" @default.
- W3104394761 title "Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors" @default.
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- W3104394761 doi "https://doi.org/10.1016/j.bmc.2020.115878" @default.
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