One-pot synthesis of tetrahydropyrimidinecarboxamides enabling in vitro anticancer activity: a combinative study with clinically relevant brain-penetrant drugs.

ABSTRACT: In this study, we describe a one-pot three-component synthesis of bioactive tetrahydopyrimidinecarboxamide derivatives employing lanthanum triflate as a catalyst. Out of the synthesized compounds, 4f had the most potent anti-cancer activity and impeded cell cycle progression effectively. Anti-cancer bioactivity was observed in 4f against liver, breast, and lung cancers as well as primary patient-derived glioblastoma cell lines. Compound 4f effectively inhibited the 3D neurosphere formation in primary patient-derived glioma stem cells. Specifically, 4f exhibited synergistic cytotoxicity with the EGFR inhibitor that is the clinical epidermal growth factor receptor inhibitor osimertinib. 4f does not exhibit anti-kinase activity and is cytostatic in nature, and further work is needed to unders

SUBMITTER: Upadhyay DB 

PROVIDER: S-EPMC11348845 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature