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Synthesis and antitumor activity of novel pyridino[2,3‐ d ]pyrimidine urea derivatives
Author(s) -
Chen Dongmei,
Chen Yumei,
Yang Di,
Zheng Zhaopeng,
Zhou Zhixu
Publication year - 2021
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.4287
Subject(s) - chemistry , pyrimidine , in vitro , urea , stereochemistry , pyridine , ic50 , pharmacology , biochemistry , medicinal chemistry , medicine
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 .