S. M. El-Sayed, M. El-Ashmawy, Said M. Bayoumi
2018
Citations
0
Influential Citations
2
Citations
Quality indicators
Journal
Journal name not available for this finding
Abstract
Abstract Objectives New hybrids of 4H-imidazole-4-one and imidazolidine-2,4-dione were designed, synthesized and evaluated for their antitumor activity in an attempt to reach an active antitumor agent with potentiated activity and selectivity toward cancerous cells. Methods Compounds 10-26 and 42-61 were synthesized and tested for their in vitro antitumor activity against prostate PC-3, colorectal HCT-116, breast MCF-7 and Hela cancer cell lines, using standard MTT assay. Key findings Compounds 12, 46 and 54 showed remarkable broad-spectrum cytotoxic potency with median IC50 nvalues of §|§zn§|¢nandn¨|©nIM, respectively. Structure-activity correlation revealed that the 4-methyl group at 3-(4-methyl-phenyl)-thiazolyl function, 4-methoxy moiety on the 5-benzyl-idene group at the 4H-imidazole-4-one and un-substituted benzoyl function at position 3- of the imidazolidine-2,4-dione favor the cytotoxic activity. Conclusions Molecular modeling study results were in-consistency with the obtained cytotoxicity results. The investigated compounds could be used as template models for further optimization.