Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution.

Andrew Potter,Victoria Oldfield,Claire Nunns,Christophe Fromont,Stuart Ray,Christopher J Northfield,Christopher J Bryant,Simon F Scrace,David Robinson,Natalia Matossova,Lisa Baker,Pawel Dokurno,Allan E Surgenor,Ben Davis,Christine M Richardson,James B Murray,Jonathan D Moore

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

Structure-guided techniques were used to evolve a 5-pyridinyl pyrazole-3-carboxylate fragment into a series of 5-aryl-carbamoyl-3-phenyl-imidazole-4-carboxylates, examples of which inhibited the Pin1 PPIase with sub-μM IC50 and blocked proliferation of prostate cancer cells.

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关键词

Pin1,Peptidyl prolyl isomerase,Fragments,Cancer

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