Open Access Original article

Monastrol mimic Biginelli dihydropyrimidinone derivatives: synthesis, cytotoxicity screening against HepG2 and HeLa cell lines and molecular modeling study

Uttara Soumyanarayanan1*, Varadaraj G Bhat1, Sidhartha S Kar1 and Jesil A Mathew2

Author Affiliations

1 Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka 576104, India

2 Department of Pharmaceutical Biotechnology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka 576104, India

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Organic and Medicinal Chemistry Letters 2012, 2:23 doi:10.1186/2191-2858-2-23

Published: 12 June 2012

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.

Keywords:
Privileged structures; Amide coupling; Mitotic kinesin; Biginelli reaction