Synthesis and in vitro study of antiproliferative benzyloxy dihydropyrimidinones

In this study, we report on antiproliferative benzyloxy dihydropyrimidinones (DHPMs) produced by the Biginelli reaction of benzyloxy benzaldehyde, urea, and diverse 1,3-diones. The reaction was catalyzed by lanthanum triflate and completed within 1-1.5 h, with 74-97% yield. The antiproliferative assay was carried out for all synthesized dihydropyrimidinones against six human solid tumor cell lines. Six compounds showed good antiproliferative activity with GI(50) values below 5 mu M. Among all the synthesized compounds, the most potent derivative showed good antiproliferative activity against all cell lines with GI(50) values in the range of 1.1-3.1 mu M. These DHPMs comply with druglikeness. Furthermore, ADMET prediction and the effect of P-glycoprotein on the antiproliferative activity were also studied. Overall, our method allows eco-friendly access to benzyloxy DHPMs as potential anticancer drugs.

Automated summary

In this study, antiproliferative benzyloxy dihydropyrimidinones (DHPMs) were successfully synthesized through the Biginelli reaction, showing good activity against human solid tumor cell lines. The most potent derivative exhibited promising antiproliferative activity with GI(50) values ranging from 1.1-3.1 μM, suggesting potential as anticancer drugs. The study also included ADMET prediction and examination of P-glycoprotein's effect on antiproliferative activity, demonstrating the eco-friendly synthesis method for potential anticancer drugs.