4.2 Article

Synthesis and anticancer activity evaluation of new 1,2,3-triazole-4-carboxamide derivatives

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MEDICINAL CHEMISTRY RESEARCH
卷 23, 期 5, 页码 2426-2438

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SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-013-0841-8

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Anticancer activity; 1,2,3-Triazole-4-carboxamide; COMPARE analysis; Molecular docking

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Anticancer screening of several novel 1,2,3-triazoles has been performed. The 1,2,3-triazole derivatives were synthesized from available starting materials according to the convenient synthetic procedures using a multicomponent reaction which gave a wide access to triazole derivatives production. The synthesized compounds were tested for their anticancer activity in NCI60 cell lines. It was observed that some compounds showed remarkable anticancer activity. Two of them possessed a significant activity on leukemia, melanoma, non-small cell lung, CNS, ovarian, renal, and breast cancer. 5-Amino-1-p-tolyl-1H-[1,2,3]triazole-4-carboxylic acid (2,5-dichloro-phenyl)-amide showed a significant correlation in COMPARE analysis. 1,2,3-triazole-4-carboxamide derivatives were synthesized in a simple and convenient synthetic path, their in vitro anticancer activity was examined after the performance of molecular docking.

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