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首页> 外文期刊>RSC Advances >Design, synthesis and pharmacological evaluation of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives as antitumor agents: in vitro and in vivo antitumor activity, cell cycle arrest and apoptotic response
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Design, synthesis and pharmacological evaluation of novel 2-chloro-3-(1H-benzo[d]imidazol-2-yl)quinoline derivatives as antitumor agents: in vitro and in vivo antitumor activity, cell cycle arrest and apoptotic response

机译：新型2-氯-3-（1H-苯并[d]咪唑-2-基）喹啉衍生物作为抗肿瘤药的设计，合成和药理评价：体内和体外抗肿瘤活性，细胞周期阻滞和凋亡反应

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摘要

A series of novel 2-chloro-3-(1 H -benzo[ d ]imidazol-2-yl)quinoline derivatives ( 3a _(1) ?3d _(6) ) were designed and synthesized as antitumor agents. In vitro antitumor assay results showed that some compounds exhibited moderate to high inhibitory activities against HepG2, SK-OV-3, NCI-H460 and BEL-7404 tumor cell lines, and most compounds exhibited much lower cytotoxicities against HL-7702 normal cell line compared to 5-FU and cisplatin. In vivo antitumor assay results showed that the representative compound 3a _(1) exhibited effective inhibition on tumor growth in the HepG2 xenograft mouse model. Mechanistic studies suggested that 3a _(1) may exert antitumor activity by the up-regulation of Bax, intracellular Ca ~(2+) release, ROS generation, p21, p27 and p53, downregulation of Bcl-2, activation of caspase-9 and caspase-3 and subsequent cleavage of PARP, and inhibition of CDK activity.
机译：设计并合成了一系列新型的2-氯-3-（1H-苯并[d]咪唑-2-基）喹啉衍生物（3a_（1）→3d_（6））作为抗肿瘤剂。体外抗肿瘤测定结果表明，某些化合物对HepG2，SK-OV-3，NCI-H460和BEL-7404肿瘤细胞系表现出中度至高抑制活性，与之相比，大多数化合物对HL-7702正常细胞系表现出低得多的细胞毒性。到5-FU和顺铂。体内抗肿瘤试验结果表明，在HepG2异种移植小鼠模型中，代表性化合物3a_（1）表现出对肿瘤生长的有效抑制作用。机理研究表明3a _（1）可能通过Bax的上调，细胞内Ca〜（2+）的释放，ROS的产生，p21，p27和p53的下调，Bcl-2的下调，caspase-9的激活而发挥抗肿瘤活性。 caspase-3和随后的PARP裂解，以及对CDK活性的抑制。

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