Synthesis of novel pyrazole – 1,2,3-triazole hybrids as anticancer agents

A series of pyrazole -1,2,3-triazole hybrids were synthesized using a metal-free catalyst in a multicomponent reaction.The new compounds were screened for its in vitro anticancer activity against A-549 and MCF-7 cell lines.The compound featuring methyl and iodo substitutions demonstrated remarkable activity, exhibiting IC50 values of 9.250.2M and 9.560.2M against A-549 and MCF-7 cells, respectively.In a similar manner, the compound featuring methoxy and bromo substitutions demonstrated enhanced activity, measuring 11.420.2M and 10.950.2M.The compound featuring bromo and iodo substituents exhibited the highest activity, with IC50 values of 13.400.3M and 12.420.2M.Evaluated their toxicity on normal human embryonic kidney cells (Hek-293) and observed no morphological changes in the cells.Additionally, a molecular docking study was conducted against the proto-oncogene c-Src, revealing a highly potent ligand that demonstrated a remarkable docking score and significant binding interactions.

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Publication Details

Journal
ARKIVOC
Published
2025-04-01
DOI
https://doi.org/10.24820/ark.5550190.p012.364
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
0.00

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article

Synthesis of novel pyrazole – 1,2,3-triazole hybrids as anticancer agents

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ARKIVOC
Synthesis and biological activity
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Synthesis of novel pyrazole – 1,2,3-triazole hybrids as anticancer agents

Rajitha Nampally, Vishnu Thumma, Ramchander Jadhav, Manohar Basude, Yadagiri Bhongiri, Hanuma Eslavath
article en

Abstract

A series of pyrazole -1,2,3-triazole hybrids were synthesized using a metal-free catalyst in a multicomponent reaction.The new compounds were screened for its in vitro anticancer activity against A-549 and MCF-7 cell lines.The compound featuring methyl and iodo substitutions demonstrated remarkable activity, exhibiting IC50 values of 9.250.2M and 9.560.2M against A-549 and MCF-7 cells, respectively.In a similar manner, the compound featuring methoxy and bromo substitutions demonstrated enhanced activity, measuring 11.420.2M and 10.950.2M.The compound featuring bromo and iodo substituents exhibited the highest activity, with IC50 values of 13.400.3M and 12.420.2M.Evaluated their toxicity on normal human embryonic kidney cells (Hek-293) and observed no morphological changes in the cells.Additionally, a molecular docking study was conducted against the proto-oncogene c-Src, revealing a highly potent ligand that demonstrated a remarkable docking score and significant binding interactions.

ARKIVOCVol. 2025(5)
Osmania University, Science and Engineering Research Board
Zero hunger
Openalex Percentile: Top 95%
Synthesis and biological activity
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