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Synthesis and antitumor activity of novel pyridino[2,3-d]pyrimidine urea derivatives
Authors:Dongmei Chen  Yumei Chen  Di Yang  Zhaopeng Zheng  Zhixu Zhou
Institution:1. School of Pharmaceutical Sciences, Guizhou University, Guiyang, PR China

Guizhou Engineering Laboratory for Synthetic Drugs, Guiyang, PR China;2. Department of Oncology, Guizhou Provincial People's Hospital, Guiyang, PR China;3. School of Pharmaceutical Sciences, Guizhou University, Guiyang, PR China

Abstract:A series of novel N-(3-((6-bromopyrido2,3-d]pyrimidin-4-yl)oxy)phenyl)pyrrolidine-1-carboxamide and 1-(3-((6-bromopyrido2,3-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 pyridine2,3-d]pyrimidine derivatives containing a urea group moieties exhibited antitumor activities against MCF-7 and HCT-116 cells in vitro.
Keywords:
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