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Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents.

Authors :
Ma, Li-Ying
Pang, Lu-Ping
Wang, Bo
Zhang, Miao
Hu, Biao
Xue, Deng-Qi
Shao, Kun-Peng
Zhang, Bao-Le
Liu, Ying
Zhang, En
Liu, Hong-Min
Source :
European Journal of Medicinal Chemistry. Oct2014, Vol. 86, p368-380. 13p.
Publication Year :
2014

Abstract

A series of novel 1,2,3-triazole-pyrimidine hybrids were designed, synthesized and evaluated for their anticancer activity against four selected cancer cell lines (MGC-803, EC-109, MCF-7 and B16-F10). Most of the synthesized compounds exhibited moderate to good activity against all the cancer cell lines selected. Compound 17 showed the most excellent anticancer activity with single-digit micromolar IC 50 values ranging from 1.42 to 6.52 μM. Further mechanism studies revealed that compound 17 could obviously inhibit the proliferation of EC-109 cancer cells by inducing apoptosis and arresting the cell cycle at G2/M phase. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
86
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
98809606
Full Text :
https://doi.org/10.1016/j.ejmech.2014.08.010