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Structure-guided design of alpha-amino acid-derived Pin1 inhibitors.

Andrew J AJ Potter, Stuart S Ray, Louisa L Gueritz, Claire L CL Nunns, Christopher J CJ Bryant, Simon F SF Scrace, Natalia N Matassova, Lisa L Baker, Pawel P Dokurno, David A DA Robinson, Allan E AE Surgenor, Ben B Davis, James B JB Murray, Christine M CM Richardson, and Jonathan D JD Moore

Bioorg Med Chem Lett 20(2):586-90 (2010) PMID 19969456

The peptidyl prolyl cis/trans isomerase Pin1 is a promising molecular target for anti-cancer therapeutics. Here we report the structure-guided evolution of an indole 2-carboxylic acid fragment hit into a series of alpha-benzimidazolyl-substituted amino acids. Examples inhibited Pin1 activity with IC(50)

DOI: 10.1016/j.bmcl.2009.11.090
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