[HTML][HTML] Synthesis and biological evaluation of benzimidazole-linked 1, 2, 3-triazole congeners as agents
KJ Harkala, L Eppakayala, TC Maringanti - Organic and Medicinal …, 2014 - Springer
KJ Harkala, L Eppakayala, TC Maringanti
Organic and Medicinal Chemistry Letters, 2014•SpringerBackground Benzimidazoles 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. Findings A simple and efficient
synthesis of triazole was carried out by treatment of 2-(4-azidophenyl)-1H-benzo [d]
imidazole (6) with different types of terminal alkynes in t-BuOH/H 2 O, sodium ascorbate, and
Zn (OTf) 2, screened for cytotoxicity assay and achieved good results. A series of new …
development of new pharmaceutical molecules and have received much attention in the last
decade because of their highly potent medicinal activities. Findings A simple and efficient
synthesis of triazole was carried out by treatment of 2-(4-azidophenyl)-1H-benzo [d]
imidazole (6) with different types of terminal alkynes in t-BuOH/H 2 O, sodium ascorbate, and
Zn (OTf) 2, screened for cytotoxicity assay and achieved good results. A series of new …
Background
Benzimidazoles 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.
Findings
A simple and efficient synthesis of triazole was carried out by treatment of 2-(4-azidophenyl)-1H-benzo[d]imidazole (6) with different types of terminal alkynes in t-BuOH/H2O, sodium ascorbate, and Zn(OTf)2, 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.
Conclusions
In 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.
Graphical Abstract
Synthesis of 1,2,3-triazole derivatives
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