2-苯并咪唑-5-羧酸乙酯衍生物的沉默调节蛋白抑制作用及抗癌活性
Sirtuin inhibition and anti-cancer activities of ethyl 2-benzimidazole-5-carboxylate derivatives.
作者信息
Yeong K Y, Nor Azizi M I H, Berdigaliyev N, Chen W N, Lee W L, Shirazi A N, Parang K
机构信息
School of Science , Monash University Malaysia , Jalan Lagoon Selatan , Bandar Sunway , 47500 , Selangor , Malaysia . Email:
Department of Biomedical and Pharmaceutical Sciences , College of Pharmacy , University of Rhode Island , Kingston , RI 02881 , USA.
出版信息
Medchemcomm. 2019 Nov 18;10(12):2140-2145. doi: 10.1039/c9md00323a. eCollection 2019 Dec 1.
Abstract
New benzimidazoles were synthesized based on the previously identified sirtuin inhibitor BZD9L1. The compounds were screened for their sirtuin (SIRT1, SIRT2 and SIRT3) inhibitory activities. Compound was determined to be a pan-SIRT1-3 inhibitor. Furthermore, the proliferation of various cancer cells was inhibited by . It was shown that elicits a cytostatic effect by inducing cell cycle arrest at the G/M phase while also showing a prominent induction of apoptosis against oral cancer cells.
摘要
基于先前鉴定出的沉默调节蛋白抑制剂BZD9L1合成了新型苯并咪唑类化合物。对这些化合物进行了沉默调节蛋白（SIRT1、SIRT2和SIRT3）抑制活性的筛选。化合物被确定为泛SIRT1 - 3抑制剂。此外，该化合物抑制了多种癌细胞的增殖。结果表明，该化合物通过诱导细胞周期停滞在G/M期发挥细胞生长抑制作用，同时对口腔癌细胞也表现出显著的凋亡诱导作用。
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