Using molecular hybridization approach, novel 18 quinoline derivatives () were designed and synthesized as EGFR-TK inhibitors. The antiproliferative activity was assessed against breast (MCF-7), leukemia (HL-60) and lung (A549) cancer cell lines. Moreover, the most active quinoline derivatives ( and ) were further investigated for their potential as EGFR-TK inhibitors. In addition, cell cycle analysis and apoptosis induction activity were conducted. A considerable cytotoxic activity was attained with IC values spanning from 0.06 to 1.12 μM. Besides, the quinoline derivatives and displayed potent inhibitory activity against EFGR with IC values of 0.18 and 0.08 μM, respectively. Accordingly, the afforded quinoline derivatives can be used as promising lead anticancer candidates for future optimization.
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| http://dx.doi.org/10.1080/17568919.2024.2342201 | DOI Listing |
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