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 prepareda series of novel triazole-conjugated dihydropyrimidinones using asynthetic 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. Here, PGP is linked to cancer.