Synthesis and in vitro study of antiproliferative benzyloxy dihydropyrimidinones
Copyright policy )Synthesis and in vitro study of antiproliferative benzyloxy dihydropyrimidinones
AbstractIn 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 GI50 values below 5 μM. Among all the synthesized compounds, the most potent derivative showed good antiproliferative activity against all cell lines with GI50 values in the range of 1.1–3.1 μM. 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.
Structure-Activity Relationship, Molecular Structure, Lanthanum, Cell Line, Tumor, Humans, Urea, Antineoplastic Agents, Pyrimidinones, Drug Screening Assays, Antitumor, Cell Proliferation
Structure-Activity Relationship, Molecular Structure, Lanthanum, Cell Line, Tumor, Humans, Urea, Antineoplastic Agents, Pyrimidinones, Drug Screening Assays, Antitumor, Cell Proliferation
selected citations These citations are derived from selected sources.This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).28 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 10%
Citations provided by BIP!Popularity provided by BIP!