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

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 IC50 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.

• Authors: Li-Ying Ma, Lu-Ping Pang, Bo Wang, Miao Zhang, Biao Hu, Deng-Qi Xue, Kun-Peng Shao, Bao-Le Zhang, Ying Liu, En Zhang, Hong-Min Liu
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 86 Pg. 368-80 (Oct 30 2014) ISSN: 1768-3254 [Electronic] France
• PMID: 25180925 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2014. Published by Elsevier Masson SAS.

Chemical References

• Antineoplastic Agents
• Pyrimidines
• Triazoles
• pyrimidine

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Apoptosis (drug effects)
• Cell Cycle (drug effects)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Dose-Response Relationship, Drug
• Drug Design
• Drug Screening Assays, Antitumor
• Humans
• MCF-7 Cells
• Molecular Structure
• Pyrimidines (chemistry, pharmacology)
• Structure-Activity Relationship
• Triazoles (chemistry, pharmacology)