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Design, Synthesis and Anticancer Activity of a New Series of N-aryl-N′-[4-(pyridin-2-ylmethoxy)benzyl]urea Derivatives
Molecules ( IF 4.2 ) Pub Date : 2021-06-08 , DOI: 10.3390/molecules26123496
Shicheng Hou 1 , Shishao Liang 1 , Chao Zhang 1 , Yingmei Han 1 , Jianhui Liang 1 , Hongyu Hu 1 , Xingeng Zhang 1 , Chun Hu 1 , Xiaoping Liu 1 , Hong Zhang 2
Affiliation  

The development of cancer treatments requires continuous exploration and improvement, in which the discovery of new drugs for the treatment of cancer is still an important pathway. In this study, based on the molecular hybridization strategy, a new structural framework with an N-aryl-N’-arylmethylurea scaffold was designed, and 16 new target compounds were synthesized and evaluated for their antiproliferative activities against four different cancer cell lines A549, MCF7, HCT116, PC3, and human liver normal cell line HL7702. The results have shown seven compounds with 1-methylpiperidin-4-yl groups having excellent activities against all four cancer cell lines, and they exhibited scarcely any activities against HL7702. Among them, compound 9b and 9d showed greatly excellent activity against the four kinds of cells, and the IC50 for MCF7 and PC3 cell lines were even less than 3μM.

中文翻译:

新系列N-芳基-N'-[4-(吡啶-2-基甲氧基)苄基]脲衍生物的设计、合成及抗癌活性

癌症治疗的发展需要不断探索和改进,其中发现治疗癌症的新药仍然是重要途径。在这项研究中,基于分子杂交策略,一个新的结构框架与N-基-N设计了'-芳甲基脲支架,合成了16个新的目标化合物,并评估了它们对四种不同癌细胞系A549、MCF7、HCT116、PC3和人肝正常细胞系HL7702的抗增殖活性。结果表明,具有 1-methylpiperidin-4-yl 基团的 7 种化合物对所有四种癌细胞系都具有优异的活性,并且它们对 HL7702 几乎没有任何活性。其中,化合物9b和9d对4种细胞均表现出极好的活性,对MCF7和PC3细胞系的IC 50甚至小于3μM。
更新日期:2021-06-08
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