Discovery of novel beta-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance
Discovery of novel beta-carboline/acylhydrazone hybrids as potent antitumor agents and overcome drug resistance
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发现新型β-咔啉/酰腙杂合物作为有效的抗肿瘤剂并克服耐药性
DOI：
10.1016/j.ejmech.2018.05.003
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发表时间：
2018
影响因子：
6.7
通讯作者：
Chen Lijuan
中科院分区：
文献类型：
--
作者：
Li Yong;Yan Wei;Yang Jianhong;Yang Zhuang;Hu Mengshi;Bai Peng;Tang Minghai;Chen Lijuan
合成了24个新的β-咔啉/酰腙杂合物并评价了它们的体外抗增殖活性。其中，1 - 2对多种癌细胞系的IC_（50）值为1-2 μM，对多药耐药癌细胞的活性最强。经处理的细胞在细胞周期的任何阶段都没有被阻止，但导致了MCF-7和MCF-7/ADR癌细胞的晚期细胞凋亡。重要的是，12 r具有一定的抗肿瘤作用，抑制肿瘤生长，毒副作用低，体重无明显下降。
Twenty-four novel β-carboline/acylhydrazone hybrids were synthesized and evaluated for theirin vitroantiproliferative activity. Among them,12rexhibited the most potent activity, with IC50values of 1–2 μM against panel of cancer cell lines and retained significant activity in multidrug resistant cancer cells. Treated cells were not arrested in any phase of cell cycle but resulted in late cellular apoptosis on both MCF-7 and MCF-7/ADR cancer cells. Importantly,12rshowed certain antitumor effect on inhibiting the tumor growth with low toxic and side effects and without significant body weight loss.