Copyright (c) 2025 Prof. Ravinder Manchal, RAJU MANNOORI, SIDDHARTHA MARUPATI, ASHOK KUMAR BAPURAM, SAIDI REDDY MODUGU
This work is licensed under a Creative Commons Attribution 4.0 International License.
Synthesis and Biological Evaluation of Quinoline-1,2,3-Triazole-Azo Hybrids as Potential EGFR Inhibitors: in vitro and in silico Approaches
Corresponding Author(s) : Ravinder Manchal
Asian Journal of Chemistry,
Vol. 37 No. 11 (2025): Vol 37 Issue 11, 2025
Abstract
In this work, the synthesis and characterization of quinolime-1,2,3-triazoles (7a-n) via azocoupling, O-propargylation and copper(I) catalyzed azide alkyne cycloaddition reactions is reported. All the synthesized compounds were evaluated for in vitro anticancer activity against human breast cancer cell lines like MDA-MB-468, MDA-MB-231 and MCF-7 and 5-fluorouracil (5-FU) as reference drug. Among all, only five compounds 7d, 7j, 7k, 7l and 7n exhibited greater activity than the standard drug 5-fluorouracil against three breast cancer cell lines with IC50 values ranging from 1.1 µM to 9.3 µM. Similarly, in vitro tyrosine kinase EGFR inhibition for the same compounds revealed that compound 7l has exhibited 2.6 times more inhibitory activity with IC50 value of 0.15 µM compared to erlotinib. Finally, in silico molecular docking on EGFR shown good binding interactions with target protein (pdb id 4HJO).
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L.K. Gediya and V.C.O. Njar, Expert Opin. Drug Discov., 4, 1099 (2009); https://doi.org/10.1517/17460440903341705
M. Szala, J.E. Nycz, G.J. Malecki, R. Sokolova, S. Ramesova, A. Switlicka-Olszewska, R. Strzelczyk, R. Podsiadly and B. Machura, Dyes Pigments, 142, 277 (2017); https://doi.org/10.1016/j.dyepig.2017.03.043
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