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ID: ALA4390709

Journal: Bioorg Med Chem Lett

Title: Design, synthesis and biological evaluation of benzimidazole derivatives as novel human Pin1 inhibitors.

Authors: Ma T, Huang M, Li A, Zhao F, Li D, Liu D, Zhao L.

Abstract: In this work, a series of novel benzimidazole derivatives were designed and synthesized as Pin1 inhibitors. Protease-coupled assay was used to investigate the Pin1 inhibitory potency of all synthesized compounds. Thirteen of them showed preferable Pin1 inhibitory effects with IC50 values lower than 5 μM, and 12a, 15b, 15d and 16c exhibited the most promising Pin1 inhibitory activity at low micromolar level (0.33-1.00 μM) than the positive control compound Juglone. Flow cytometry results showed that treating PC-3 cells with 16c caused slight cycle arrest in a concentration-dependent manner. The structure-activity relationships of R1, R2, R3 and linker of the benzimidazole derivatives were analyzed in detail, which would help further exploration of new Pin1 inhibitors.

CiteXplore: 31103446

DOI: 10.1016/j.bmcl.2018.11.045