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Background and the purpose of the study  A common approach in cancer chemotherapy is development of drugs that interrupt the mitosis phase of cell division. Dimethylenastron is a known kinesin inhibitor. In this study, six novel dimethylenastron analogues ( 4a-f ), in which 3-hydroxyphenyl substituent has been replaced with substituted benzylimidazolyl, were synthesized through Biginelli reaction.    Methods  Six novel Biginelli compounds  (4a-f)  were synthesized through one step Biginelli reaction of imidazole aldehydes ( 3a-c ), dimedone and urea or thioura. In vitro cytotoxicities of prepared compounds were investigated using MTT assay. Furthermore the ELIPA kit was implemented to study inhibitory effects of synthesized compounds on ATPase activity of kinesin by measuring of organic phosphate.    Results  Our results indicated that analogue  4c  is the most toxic and analogues  4f ,  4b  and dimethylenasteron were less cytotoxic in compare with other analogues. On the other hand, analogue  4a ,  4b ,  4c  and  4e  showed stronger Kinesin inhibition as compared with analogue  4f  and dimethylenasteron. None of synthesized compounds were as potent kinesin inhibitor as Taxol. Docking analysis revealed that hydrogen bond formation and hydrophobic interactions were the key factors affecting inhibitory effects of these compounds.    Conclusion  Newly synthesized compounds were found to have moderate to good cytotoxicity against HeLa cancer cell. Our results may be helpful in further design of dihydropyrimidine as potential anticancer agents.

Synthesis and molecular modeling of six novel monastrol analogues: evaluation of cytotoxicity and kinesin inhibitory activity against HeLa cell line