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

A Potter, V Oldfield, C Nunns, C Fromont, S Ray…

文献索引：Potter, Andrew; Oldfield, Victoria; Nunns, Claire; Fromont, Christophe; Ray, Stuart; Northfield, Christopher J.; Bryant, Christopher J.; Scrace, Simon F.; Robinson, David; Matossova, Natalia; Baker, Lisa; Dokurno, Pawel; Surgenor, Allan E.; Davis, Ben; Richardson, Christine M.; Murray, James B.; Moore, Jonathan D. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 22 p. 6483 - 6488

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被引用次数: 43

摘要

Pin1 is an emerging oncology target strongly implicated in Ras and ErbB2-mediated tumourigenesis. Pin1 isomerizes bonds linking phospho-serine/threonine moieties to proline enabling it to play a key role in proline-directed kinase signalling. Here we report a novel series of Pin1 inhibitors based on a phenyl imidazole acid core that contains sub-μM inhibitors. Compounds have been identified that block prostate cancer cell growth under ...