Pediatric Infectious Diseases: Open Access

Synthesis, in vitro Anticancer and Antimicrobial Evaluation of Novel Substituted Dihydropyrimidines

Objective:To synthesize new dihydropyrimidine derivatives and check their anticancer, antibacterial and antifungal activities.

Methods:A series of 1,4-dihydropyrimidine derivatives were prepared from Biginelli reactions by using ethyl acetoacetate, substituted benzaldehyde and thiourea in the presence of piperidine and ethanol. The compounds were reacted with dimethylsulphate, diethylsulphate, butyl bromide and benzyl chloride to give the new series of compounds. The structures of the newly synthesized compounds were established by IR, 1H NMR, Mass spectra and elemental analysis. The synthesized compounds were evaluated for theirin-vitroanticancer activity by using SRB assay method against the growth of fourhumans cancer cell lines, antibacterial activity against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coliand for antifungal activity against Candida albicansand Aspergillus niger.

Results:The compounds exhibited good anticancer activity and moderate antibacterial and antifungal activities.Some of these dihydropyrimidine derivatesshowed significant anticancer activity when compared with the doxorubicin as a standard reference drug.

Conclusion:The results of anticancer activity evaluation demonstrated that the in vitroanticancer effect of some of the synthesized compounds are significant, however still there is a need for further exploration of these for other synthetic & biological possibilities so that this skeleton can be used as a novel anticancer scaffold for further modification and design of novel potent compounds.

Author(s):

Kulbhushan Rana, S. D. College Barnala, Punjabi University , Punjab, India

Abstract | PDF

Share this