Abstract
Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized. IC50 values of the synthesized compounds against the proliferation of human hepatocellular carcinoma and human epithelial carcinoma cell lines were determined through MTT assay. Molecular docking study gave a clear insight into the structural activity relationship of the compounds in comparison with monastrol.
Highlights
Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized
This paper describes the synthesis and evaluation of monastrol-related racemic dihydropyrimidinones substituted with privileged structures [9] like pyrrolidine, piperidine and morpholine through an amide linkage
A series of 12 novel monastrol analogs based on Biginelli reaction were synthesized with concentration at 50% inhibition (IC50) in the range of 120 to 398 μg/mL against human hepatocellular carcinoma (HeLa) and human epithelial carcinoma (HepG2) cell lines
Summary
Biginelli dihydropyrimidinone derivatives as structural analogs of monastrol, a known human kinesin Eg5 inhibitor, were synthesized. Recent progress in the DHPM class of the anticancer agent monastrol, an inhibitor of human kinesin Eg5 [1,2], has led to the attention for efficient pharmacophore variation of Biginelli DHPMs. Human kinesin Eg5 plays a crucial role in bipolar spindle generation during mitosis, inhibition of which leads to mitotic arrest and subsequent apoptotic cell death [3]. Human kinesin Eg5 plays a crucial role in bipolar spindle generation during mitosis, inhibition of which leads to mitotic arrest and subsequent apoptotic cell death [3] It is considered as one of the promising targets in cancer chemotherapy.
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