Synthesis and biological evaluation of benzimidazole-linked 1,2,3-triazole congeners as agentsReport as inadecuate

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Organic and Medicinal Chemistry Letters

, 4:14

First Online: 02 December 2014Received: 14 October 2014Accepted: 30 October 2014


BackgroundBenzimidazoles and triazoles are useful structures for research and development of new pharmaceutical molecules and have received much attention in the last decade because of their highly potent medicinal activities.

FindingsA simple and efficient synthesis of triazole was carried out by treatment of 2-4-azidophenyl-1H-benzodimidazole 6 with different types of terminal alkynes in t-BuOH-H2O, sodium ascorbate, and ZnOTf2, screened for cytotoxicity assay and achieved good results. A series of new benzimidazole-linked 1,2,3-triazole 8a-i congeners were synthesized through cyclization of terminal alkynes and azide. These synthesized congeners 8a-i were evaluated for their cytotoxicity against five human cancer cell lines. These benzimidazole-linked 1,2,3-triazole derivatives have shown promising activity with IC50 values ranging from 0.1 to 43 μM. Among them, the compounds 8a , 8b , 8c , and 8e showed comparable cytotoxicity with adriamycin control drug.

ConclusionsIn conclusion, we have developed a simple, convenient, and an efficient convergent approach for the synthesis of benzimidazole-linked 1,2,3-triazole congeners as agents.

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AbstractSynthesis of 1,2,3-triazole derivatives

KeywordsBenzimidazole Clic reaction Cytotoxicity Electronic supplementary materialThe online version of this article doi:10.1186-s13588-014-0014-x contains supplementary material, which is available to authorized users.

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Author: Karna Ji Harkala - Laxminarayana Eppakayala - Thirumala Chary Maringanti



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