SYNTHESIS, In-vitro CYTOTOXICITY AND IN SILICO INVESTIGATIONS OF QUINAZOLINONE INTEGRATED CHALCONES: AS NOVEL POTENTIAL DUAL-TARGETING ANTICANCER AGENTS TO TREAT LUNG CANCER AND COLORECTAL CANCER

• Published in: Rasāyan journal of chemistry 2023-07, Vol.16 (3), p.1104-1115
• Main Authors: Arora, P. K., S. Kumar, Bansal, S. K., Sharma, P. C.
• Format: Article
• Language: English
• ISSN: 0974-1496; 0974-1496
• DOI: 10.31788/RJC.2023.1638343

The present study focuses on the synthesis of some 2-methoxyphenylquinazolin-4-one incorporated chalcone hybrids to evaluate their cytotoxic potential by MTT assay, and their affinity to bind with T790M mutated epidermal growth factor receptor (EGFR; protein data bank Id: 5Y9T) and G12D mutated Kirsten rat sarcoma (K-RAS; protein data bank Id:4EPT) by molecular docking (auto dock-4) by employing validated docking parameters. Against the lung cancer cells (A549), except C7 (IC50: 48.22 g/ml), the other title compounds exhibited more cytotoxicity (IC50 16.88g/ml to 33.98g/ml) than the erlotinib (reference). Against the colorectal cancer cells, the compound C4 (IC50: 9.74 g/ml) exhibited more cytotoxicity than the reference (IC50: 16.13 g/ml). For the normal cell lines (Vero), the compound C1 (IC50 27.88g/ml) is less toxic to normal cells, than the reference. The title compounds can be a boon for the development of smart anticancer drugs with dual target virtue