Hexahydroquinoline (HHQ) scaffold was constructed and recruited for development of new series of anticancer agents. Thirty-two new compounds were synthesised where x-ray crystallography was performed to confirm enantiomerism. Thirteen compounds showed moderate to good activity against NCI 60 cancer cell lines, with GI % mean up to 74% for . Expending erlotinib as a reference drug, target compounds were verified for their inhibiting activities against EGFR, EGFR, and EGFR where compound was the best inhibitor with IC = 0.097, 0.280, and 0.051 µM, respectively, compared to erlotinib (IC = 0.082 µM, 0.342 µM, and 0.055 µM, respectively). Safety profile was validated using normal human lung (IMR-90) cells. and disrupted cell cycle at pre-G1 and G2/M phases in lung cancer, HOP-92, and cell line. Molecular docking study was achieved to understand the potential binding interactions and affinities in the active sites of three versions of EGFRs.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10408569PMC
http://dx.doi.org/10.1080/14756366.2023.2241674DOI Listing

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