Novel Approaches for the Solid-Phase Synthesis of Dihydroquinazoline-2(1H)-One Derivatives and Biological Evaluation as Potential Anticancer Agents.

ABSTRACT: In the design of antineoplastic drugs, quinazolinone derivatives are often used as small molecule inhibitors for kinases or receptor kinases, such as the EGFR tyrosine kinase inhibitor gefitinib, p38MAP kinase inhibitor DQO-501, and BRD4 protein inhibitor PFI-1. A novel and convenient approach for the solid-phase synthesis of dihydroquinazoline-2(1H)-one derivatives was proposed and 19 different compounds were synthesized. Cytotoxicity tests showed that most of the target compounds had anti-proliferative activity against HepG-2, A2780 and MDA-MB-231 cell lines. Among them, compounds CA1-e and CA1-g had the most potent effect on A2780 cells, with IC₅₀ values of 22.76 and 22.94 μM, respectively. In addition, in an antioxidant assay, the IC₅₀

SUBMITTER: Wang Q 

PROVIDER: S-EPMC9737648 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature