Novel Dihydropyrimidinone Derivatives as Potential P-Glycoprotein Modulators.

ABSTRACT: P-glycoprotein (Pgp), an ATP binding cassette (ABC) transporter, is an ATP-dependent efflux pump responsible for cancer multidrug resistance. As part of efforts to identify human Pgp (hPgp) inhibitors, we prepared a series of novel triazole-conjugated dihydropyrimidinones using a synthetic approach that is well suited for obtaining compound libraries. Several of these dihydropyrimidinone derivatives modulate human P-glycoprotein (hPgp) activity with low micromolar EC₅₀ values. Molecular docking studies suggest that these compounds bind to the M-site of the transporter.

SUBMITTER: Bijani S 

PROVIDER: S-EPMC9118204 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature