Synthesis and evaluation of novel benzimidazole derivatives as sirtuin inhibitors with antitumor activities
Synthesis and evaluation of novel benzimidazole derivatives as sirtuin inhibitors with antitumor activities
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DOI：
10.1016/j.bmc.2013.12.029
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发表时间：
2014-01-15
影响因子：
3.5
通讯作者：
Shirazi, Amir Nasrolahi
中科院分区：
文献类型：
--
作者：
Yoon, Yeong Keng;Ali, Mohamed Ashraf;Shirazi, Amir Nasrolahi
设计、合成了15个新型苯并咪唑类化合物，并对其SIRT 1和SIRT 2抑制活性进行了评价。与SIRT 1相比，所有化合物对SIRT 2显示出更好的抑制作用。在这些化合物中，化合物5 j显示出对SIRT 1（IC 50 = 58.43 μ M）以及SIRT 2（IC 50 = 45.12 μ M）的最佳抑制活性。细胞毒性试验表明化合物5 j对两种不同的乳腺癌细胞株（MCF-7和MDA-MB-468）具有良好的抗肿瘤活性。对新合成的苯并咪唑类化合物进行了简单的构效关系研究。(C)2013爱思唯尔有限公司保留所有权利。
A total of 15 novel benzimidazole derivatives were designed, synthesized and evaluated for their SIRT1 and SIRT2 inhibitory activity. All compounds showed better inhibition on SIRT2 as compared to SIRT1. Among these, compound 5j displayed the best inhibitory activity for SIRT1 (IC50 = 58.43 mu M) as well as for SIRT2 (IC50 = 45.12 mu M). Cell cytotoxicity assays also showed that compound 5j possesses good antitumor activity against two different cancer cell lines derived frombreast cancer (MCF-7 and MDA-MB-468). A simple structure-activity-relationship (SAR) study of the newly synthesized benzimidazole derivatives was also discussed. (C) 2013 Elsevier Ltd. All rights reserved.