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.
Authors
- Rajitha Nampally
- Vishnu Thumma (ORCID: https://orcid.org/0000-0001-6830-3671)
- Ramchander Jadhav
- Manohar Basude (ORCID: https://orcid.org/0000-0002-5433-0529)
- Yadagiri Bhongiri
- Hanuma Eslavath
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
Funders
- Osmania University
- Science and Engineering Research Board