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Design and Synthesis of Novel quinoline/chalcone/1,2,4-triazole hybrids as potent antiproliferative agent targeting EGFR and BRAFV600E kinases

مؤلف البحث
Aliaa M. Mohassab, Heba A. Hassan, Dalia Abdelhamid, Ahmed M. Gouda, Bahaa G. M. Youssif, Hiroshi Tateishi, Mikako Fujita, Masami Otsuka, Mohamed Abdel-Aziz.
مجلة البحث
Bioorganic Chemistry
الناشر
elsevier
تصنيف البحث
1
عدد البحث
Vol 106
موقع البحث
https://doi.org/10.1016/j.bioorg.2020.104510
سنة البحث
2020
المشارك في البحث
ملخص البحث

New quinoline / chalcone hybrids containing 1,2,4-triazole moiety have been designed, synthesized and their structures elucidated and confirmed by various spectroscopic techniques. The designed compounds showed moderate to good activity on different NCI 60 cell lines in a single-dose assay with a growth inhibition rate ranging from 50% to 94%. Compounds 7b, 7d, 9b, and 9d were the most active compounds in most cancer cell lines with a growth inhibition percent between 77% and 94%. Newly synthesized hybrids were evaluated for their anti-proliferative activity against a panel of four human cancer cell lines. Compounds 7a, 7b, 9a, 9b, and 9d showed promising antiproliferative activities. These compounds were further tested for their inhibitory potency against EGFR and BRAFV600E kinases with erlotinib as a reference drug. The molecular docking study of compounds 7a, 7b, 9a, 9b, and 9d revealed nice fitting into the active site of EGFR and BRAFV600E kinases. Compounds 7b, 9b, and 9d displayed the highest binding affinities and similar binding pattern to those of erlotinib.