南美超级胎牛血清999尝鲜特惠
β-咔啉衍生物作为靶向自噬的抗肿瘤药物的设计合成与药理评价
Design, synthesis and pharmacological evaluation of β-carboline derivatives as potential antitumor agent via targeting autophagy
Jingsheng Ao, Feng Zeng, Longhao Wang, Liqin Qiu, Rihui Cao, Xiangpan Li
Journal：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
IF：7.09
DOI：10.1016/j.ejmech.2022.114955
PMID：36459757
Published：2022-11-26
research field：肿瘤学分子生物学药理学药物化学生物化学
Abstract
A series of novel β-carboline derivatives was designed, synthesized and evaluated as potential anticancer agents . Among them, compound 6g showed the most potent antiproliferative activity against the 786–0, HT-29 and 22RV1 cell lines with IC 50 values of 2.71, 2.02, and 3.86 μM, respectively. The antitumor efficiency of compound 6g in vivo was also evaluated, and the results revealed that compound 6g significantly suppressed tumor development and reduced tumor weight in a mouse colorectal cancer homograft model. Further investigation on mechanisms of action demonstrated that compound 6g inhibited HCT116 cell growth by stimulating the ATG5/ATG7-dependent autophagic pathway. These molecules might be served as candidates for further development of colorectal cancer therapy agent.
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