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¨|©nİM, 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.
Key words: Key-words: Synthesis, imidazolidine-2,4-dione, 4H-imidazole-4-one, Cytotoxic activity, Molecular modeling study.
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