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

• A series of novel 1,2,3-triazole-pyridimine hybrids were synthesized.
• Several compounds were more potent than 5-fluorouracil against EC-109, MCF-7 and MGC-803.
• Compound 17 was highly selective in its cytotoxicity activity.
• Compound 17 showed cell cycle arrest at G2/M phase and induced apoptosis.

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.

Novel 1,2,3-triazole-pyridimine hybrids 17 exhibited about 7 fold more potent than 5-Fu against EC-109.Figure optionsDownload as PowerPoint slide