Copyright (c) 2024 Begum Alia, Farveen MD, Sreelatha G
This work is licensed under a Creative Commons Attribution 4.0 International License.
Design and Synthesis of Quinazoline Bearing Thiazolotriazole Scaffolds as Potent EGFR Inhibitor for Anti-Breast Cancer Activity
Corresponding Author(s) : Alia Begum
Asian Journal of Chemistry,
Vol. 37 No. 1 (2025): Vol 37 Issue 1, 2025
Abstract
A number of fused heterocyclic hybrids with central rings of thiazolotriazoles are synthesized and characterized by 1H NMR, 13C NMR and EI-MS techniques. The synthesized compounds showed variable degrees of efficacy in their in vitro cytotoxic activity against MCF-7, MDA-MB-231 and MCF-10A cell lines. Remarkably some analogues exhibited greater activity than the reference drugs, erlotinib. The most effective compounds, 6i, 6h and 6j, displayed significant EGFR tyrosine kinase inhibition and significant cytotoxicity, in accordance with the molecular docking investigations that revealed favourable binding contacts and energies inside the EGFR active region.
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- https://www.rcsb.org/structure/4HJO
References
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P. Kumar, A. Kumar and J.K. Makrandi, J. Heterocycl. Chem., 50, 1223 (2013); https://doi.org/10.1002/jhet.1600
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M. Kumsi, B. Poojary, P.L. Lobo, N.S. Kumari and A. Chullikana, Z. Naturforsch. B, 65, 1509 (2010); https://doi.org/10.1515/znb-2010-1215
T. Krishnaraj and S. Muthusubramanian, J. Heterocycl. Chem., 52, 1314 (2015); https://doi.org/10.1002/jhet.2161
A.E. Maennling, M.K. Tur, M. Niebert, T. Klockenbring, F. Zeppernick, S. Gattenlöhner, I. Meinhold-Heerlein and A.F. Hussain, Cancers, 11, 1826 (2019); https://doi.org/10.3390/cancers11121826
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