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. 2024;16(11):1087-1107.
doi: 10.1080/17568919.2024.2342201. Epub 2024 May 9.

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

Noha Ryad  1 , Ayman Abo Elmaaty  2 , Ibrahim M Ibrahim  3 , Ali Hassan Ahmed Maghrabi  4 , Maryam Abdulrahman Yahya Alahdal  4 , Rasha Mohammed Saleem  5 , Islam Zaki  6 , Lina M A Abdel Ghany  7
Affiliations

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

Noha Ryad et al. Future Med Chem. 2024.

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.

Keywords: ADMET; EGFR; SAR; anti-proliferative; molecular docking; molecular hybridization; quinoline.

Plain language summary

[Box: see text].

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Conflict of interest statement

The authors have no competing interests or relevant affiliations with any organization or entity with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

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References

    1. Curado MP, Voti L, Sortino-Rachou AM. Cancer registration data and quality indicators in low and middle income countries: their interpretation and potential use for the improvement of cancer care. Cancer Caus. Control. 2009;20:751–756. doi:10.1007/s10552-008-9288-5 - DOI - PubMed
    1. Torre LA, Bray F, Siegel RL, et al. . Global cancer statistics, 2012. CA: A. Cancer J. Clin. 2015;65:87–108. doi:10.3322/caac.21262 - DOI - PubMed
    1. Demaria M, O'Leary MN, Chang J, et al. . Cellular senescence promotes adverse effects of chemotherapy and cancer relapse. Cancer Discov. 2017;7:165–176. doi:10.1158/2159-8290.cd-16-0241 - DOI - PMC - PubMed
    1. Chang J, Ren H, Zhao M, et al. . Development of a series of novel 4-anlinoquinazoline derivatives possessing quinazoline skeleton: Design, synthesis, EGFR kinase inhibitory efficacy, and evaluation of anticancer activities in vitro. Eur. J. Med. Chem. 2017;138:669–688. doi:10.1016/j.ejmech.2017.07.005 - DOI - PubMed
    1. Kasture VS, Musmade DS, Aher SJ, et al. . Tyrosine kinases: promising targets for cancer chemotherapy. Med. Chem. Drug Discov. 2012;2:37–51. doi:10.3390/ijms222111659 - DOI

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