Design, Synthesis, Characterization, Molecular Docking Studies of Novel Quinazolinone Derivatives as Potential EGFR Inhibitors (Research Article)

Author(s): A.Jyothsna, K.Padma Latha

Abstract: A series of some novel quinazolinone derivatives III-3(a-j) were synthesized by a conventional method via cyclization and Schiff’s base mechanism. All the synthesized compounds gave a good yield between 78-86%. Final structure was confirmed by FT-IR, LC-MASS and 1H NMR analytical data. The novel Quinazolinone derivatives (III-3a-3j) are screened for anticancer activity against MCF-7, SKVO3 Cell lines by MTT assay method. From the resulting data, the compound III-3i (IC50 value of 0.035 μM against MCF-7 and 0.1 μM against SKVO3) exhibited good anticancer activity compared with Doxorubicin as standard. The molecular docking studies of these novel Qunazolinone showed good agreement with the biological results their binding pattern and affinity towards the active site of EGFR was examination.

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