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Synthesis and antitumor activity of novel pyridino[2,3-d]pyrimidine urea derivatives
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2021-05-05 , DOI: 10.1002/jhet.4287
Dongmei Chen 1, 2 , Yumei Chen 1, 2 , Di Yang 1, 2 , Zhaopeng Zheng 3 , Zhixu Zhou 1, 2, 4
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A series of novel N-(3-((6-bromopyrido[2,3-d]pyrimidin-4-yl)oxy)phenyl)pyrrolidine-1-carboxamide and 1-(3-((6-bromopyrido[2,3-d]pyrimidin-4-yl)oxy)phenyl)-3-propylurea derivatives were synthesized. Their antitumor activities against human breast carcinoma cells (MCF-7) and human colon cancer cells (HCT-116) in vitro were evaluated, using sorafenib as a positive control drug. Anticancer bioassays indicated that several compounds exhibited appreciable anticancer activity against MCF-7 and HCT-116 cells. Particularly, compounds 9g and 8b demonstrated the most significant inhibitory effect against HCT-116 and MCF-7 cells, with inhibition ratios of 25.56% and 26.46%, respectively. Additionally, the synthesized pyridine[2,3-d]pyrimidine derivatives containing a urea group moieties exhibited antitumor activities against MCF-7 and HCT-116 cells in vitro.

中文翻译:

新型吡啶并[2,3-d]嘧啶脲衍生物的合成及抗肿瘤活性

一系列新型N- (3-((6-溴吡啶并[2,3- d ]嘧啶-4-基)氧基)苯基)吡咯烷-1-甲酰胺和1-(3-((6-溴吡啶并[2, 3- d合成]嘧啶-4-基)氧基)苯基)-3-丙基脲衍生物。使用索拉非尼作为阳性对照药物,评估了它们在体外对人乳腺癌细胞 (MCF-7) 和人结肠癌细胞 (HCT-116) 的抗肿瘤活性。抗癌生物测定表明,几种化合物对 MCF-7 和 HCT-116 细胞表现出明显的抗癌活性。特别是化合物9g8b对 HCT-116 和 MCF-7 细胞的抑制作用最为显着,抑制率分别为 25.56% 和 26.46%。此外,合成的含有脲基部分的吡啶[2,3- d ]嘧啶衍生物在体外对MCF-7和HCT-116细胞具有抗肿瘤活性。
更新日期:2021-05-05
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