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Harnessing molecular hybridization approach to discover novel quinoline EGFR-TK inhibitors for cancer treatment.

ABSTRACT: Aim: Using molecular hybridization approach, novel 18 quinoline derivatives (6a-11) were designed and synthesized as EGFR-TK inhibitors. Materials & methods: The antiproliferative activity was assessed against breast (MCF-7), leukemia (HL-60) and lung (A549) cancer cell lines. Moreover, the most active quinoline derivatives (6d and 8b) were further investigated for their potential as EGFR-TK inhibitors. In addition, cell cycle analysis and apoptosis induction activity were conducted. Results: A considerable cytotoxic activity was attained with IC50 values spanning from 0.06 to 1.12 μM. Besides, the quinoline derivatives 6d and 8b displayed potent inhibitory activity against EFGR with IC50 values of 0.18 and 0.08 μM, respectively. Conclusion: Accordingly, the afforded quinoline derivatives can be used as promising lead anticancer candidates for future optimization.

SUBMITTER: Ryad N 

PROVIDER: S-EPMC11216632 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature

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Harnessing molecular hybridization approach to discover novel quinoline EGFR-TK inhibitors for cancer treatment.

Ryad Noha N   Elmaaty Ayman Abo AA   M Ibrahim Ibrahim I   Ahmed Maghrabi Ali Hassan AH   Yahya Alahdal Maryam Abdulrahman MA   Saleem Rasha Mohammed RM   Zaki Islam I   Ghany Lina M A Abdel LMAA  

Future medicinal chemistry 20240509 11

<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 a  ...[more]

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