biostudies-literatureUnknown16(11)Ryad N<b>Aim:</b> Using molecular hybridization approach, novel 18 quinoline derivatives (<b>6a-11</b>) were designed and synthesized as EGFR-TK inhibitors. <b>Materials & methods:</b> The antiproliferative activity was assessed against breast (MCF-7), leukemia (HL-60) and lung (A549) cancer cell lines. Moreover, the most active quinoline derivatives (<b>6d</b> and <b>8b</b>) were further investigated for their potential as EGFR-TK inhibitors. In addition, cell cycle analysis and apoptosis induction activity were conducted. <b>Results:</b> A considerable cytotoxic activity was attained with IC₅₀ values spanning from 0.06 to 1.12 μM. Besides, the quinoline derivatives <b>6d</b> and <b>8b</b> displayed potent inhibitory activity against EFGR with IC₅₀ values of 0.18 and 0.08 μM, respectively. <b>Conclusion:</b> Accordingly, the afforded quinoline derivatives can be used as promising lead anticancer candidates for future optimization.Future medicinal chemistry1087-1107https://www.ebi.ac.uk/biostudies/studies/S-EPMC11216632biostudies-literatureHarnessing molecular hybridization approach to discover novel quinoline EGFR-TK inhibitors for cancer treatment.PMC11216632Saleem RMElmaaty AAZaki IAhmed Maghrabi AHRyad NM Ibrahim IYahya Alahdal MAGhany LMAAfalseHarnessing molecular hybridization approach to discover novel quinoline EGFR-TK inhibitors for cancer treatment.<b>Aim:</b> Using molecular hybridization approach, novel 18 quinoline derivatives (<b>6a-11</b>) were designed and synthesized as EGFR-TK inhibitors. <b>Materials & methods:</b> The antiproliferative activity was assessed against breast (MCF-7), leukemia (HL-60) and lung (A549) cancer cell lines. Moreover, the most active quinoline derivatives (<b>6d</b> and <b>8b</b>) were further investigated for their potential as EGFR-TK inhibitors. In addition, cell cycle analysis and apoptosis induction activity were conducted. <b>Results:</b> A considerable cytotoxic activity was attained with IC₅₀ values spanning from 0.06 to 1.12 μM. Besides, the quinoline derivatives <b>6d</b> and <b>8b</b> displayed potent inhibitory activity against EFGR with IC₅₀ values of 0.18 and 0.08 μM, respectively. <b>Conclusion:</b> Accordingly, the afforded quinoline derivatives can be used as promising lead anticancer candidates for future optimization.2024-01-01T00:00:00Z20242026-06-02T20:46:53.676Z2026-04-20T03:14:21.784ZS-EPMC112166323872223510.1080/17568919.2024.2342201