Synthesis and evaluation of novel benzimidazole derivatives as sirtuin inhibitors with antitumor activities.
作者： Yeong Keng Yoon , Mohamed Ashraf Ali , Ang Chee Wei , Tan Soo Choon , Hasnah Osman
DOI: 10.1016/J.BMC.2013.12.029
关键词:
摘要: A total of 15 novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 SIRT2 inhibitory activity. All compounds showed better inhibition on as compared to SIRT1. Among these, compound 5j displayed the best activity (IC50=58.43μM) well (IC50=45.12μM). Cell cytotoxicity assays also that possesses good antitumor against two different cancer cell lines derived from breast (MCF-7 MDA-MB-468). simple structure-activity-relationship (SAR) study newly was discussed.
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