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Abstract
AbstractCancer is one of the leading causes of death worldwide, and it has a major impact on public health. Phosphatidylinositol 3‐kinase (PI3Kα) has been recognized as a promising drug target for developing anticancer agents. Herein, a series of N‐phenyl‐6‐fluoro‐4‐hydroxy‐2‐quinolone‐3‐carboxamides was developed to target PI3Kα. All synthesized compounds were characterized using FT‐IR, NMR (1H and 13C) and elemental analysis. All synthesized chemical analogues exerted distinctive anticancer activity. They inhibited the growth of human epithelial colorectal adenocarcinoma (Caco‐2) with IC50 values between 48.63–378 μM, and human colon cancer (HCT‐116) cell lines with IC50 values between 44–664 μM. Computational modelling studies provided important biological insight. Induced‐fit docking (IFD) studies showed that the synthesized chemical analogues fit the kinase catalytic domains and form a significant H‐bond interaction network with key amino acids at the biding site. Furthermore, cheminformatics analyses indicated that all synthesized compounds were drug‐like permitting further animal testing or clinical development.
Published Version
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