Synthesis and anti-proliferative activity of some new quinoline based 4,5-dihydropyrazoles and their thiazole hybrids as EGFR inhibitors |
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| Institution: | 1. Department of Chemistry, National Institute of Technology, Warangal, 506004, Telangana, India;2. Department of Biotechnology, National Institute of Technology, Warangal, 506004, Telangana, India;3. Environmental Monitoring & Exposure Assessment (Air) Laboratory, ICMR?NIREH, Bhopal, 462030, Madhya Pradesh, India;4. Molecular Modeling and Medicinal Chemistry Group, Department of Chemistry, University College of Science, Osmania University, Hyderabad, 500007, Telangana, India |
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| Abstract: | Quinoline derivatives 2, 3, quinolinyl based pyrazolines 4a,b, 5 and quinolinyl pyrazolinyl thiazole hybrids 6a-d, 7a-c and 8a-d were synthesized and screened for their anti-proliferative activity against MCF-7, HeLa and DLD1 cancer cell lines as well as normal fibroblast WI-38. Most of the tested compounds showed promising anticancer activity in addition to their safety towards the normal cell line. Eight compounds eliciting superior cytotoxicity against DLD1 and safe to the normal cell line 2, 3, 5, 6a, 6b, 7b, 7c and 8a were evaluated for their efficacy as EGFR inhibitors. They revealed inhibitory activity at nanomolar level especially compounds 6b, 2 and 7c with IC50 (31.80, 37.07 and 42.52 nM) in comparison to Gefitinib (IC50 = 29.16 nM). |
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| Keywords: | Quinoline Pyrazoline Thiazole EGFR Anticancer |
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