Du, Lifei; Wang, Xiaoyu; Cui, Guonan; Xu, Bailing published the artcile< Design, synthesis and biological evaluation of novel thiazole-based derivatives as human Pin1 inhibitors>, Recommanded Product: tert-Butyl piperazine-1-carboxylate hydrochloride, the main research area is thiazole based derivative human Pin1 inhibitors; PPIase; Pin1; Pin1 inhibitor; Thiazole derivatives.
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 0.95μM. The structure-activity relationship (SAR) and mol. modeling study indicated that introducing an alicyclic ring with an H-bond acceptor would be a viable way to improve the binding affinity.
Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 76535-74-5 belongs to class piperazines, and the molecular formula is C9H19ClN2O2, Recommanded Product: tert-Butyl piperazine-1-carboxylate hydrochloride.
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics