Concise synthesis and biological activity evaluation of novel pyrazinyl-aryl urea derivatives against several cancer cell lines, which can especially induce T24 apoptotic and necroptotic cell death
Concise synthesis and biological activity evaluation of novel pyrazinyl-aryl urea derivatives against several cancer cell lines, which can especially induce T24 apoptotic and necroptotic cell death
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新型吡嗪基芳基脲衍生物的简明合成和生物活性评价，对多种癌细胞系，尤其是诱导 T24 细胞凋亡和坏死性细胞死亡
DOI：
10.1039/d1md00306b
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发表时间：
2021-11-11
影响因子：
4.1
通讯作者：
Wei, Ying
中科院分区：
文献类型：
--
作者：
Chen, Jia-Nian;Chen, Chu-Ting;Wei, Ying
在瑞戈非尼结构修饰的基础上，合成了28个吡嗪基芳基脲衍生物，并对其体外抗增殖活性进行了评价。6个化合物（5-16、5-17、5-18、5-19、5-22和5-23）对人膀胱癌T24细胞系表现出良好的抑制活性，并且5-23表现出最强的抑制活性（IC 50 = 4.58 +/-0.24 μ M），具有高选择性。化合物5-23在低浓度范围（
Based on the structural modification of regorafenib, 28 pyrazinyl-aryl urea derivatives were synthesized and their in vitro antiproliferative activities were evaluated. Six compounds (5-16, 5-17, 5-18, 5-19, 5-22, and 5-23) exhibited favorable inhibitory activity against the human bladder cancer T24 cell line, and 5-23 demonstrated the strongest inhibitory activity (IC50 = 4.58 +/- 0.24 mu M) with high selectivity. Compound 5-23 induced apoptosis in the low concentration range (