ABSTRACT
Objective Using Ex-Rad as a lead compound to design and synthesize aroyl derivatives with protein tyrosine kinases(PTK) inhibitiory activity. Methods 1-[(4-Fluorophenyl)amioncarbonyl] cyclopropanecarboxylic acid, and 2-oxo-1-phenylimidazolidine were used as raw materials to synthesize intermediates 3a-3d, respectively. The target compounds T1-T7 were synthesized by chloroformylation reaction with 3a-3d. Enzyme-linked immunosorbent assay (ELISA) was used and inhibitory rate was calculated to screen out the compounds with PTK inhibitory activity. Results Seven new compounds containing aroyl groups were synthesized and their structures were confirmed by 1H NMR. The evaluation of the seven compounds demonstrated that PTK inhibitory activity of T2 and T6 were stronger than that of the lead compound. Conclusion The synthetic method is simple, and the materials are cheap and readily available. T2 and T6 show strong PTK inhibitory activity by ELISA.
ABSTRACT
Objective Using Ex-Rad as a lead compound to design and synthesize aroyl derivatives with protein tyrosine ki?nases(PTK)inhibitiory activity. Methods 1-[(4-Fluorophenyl)amioncarbonyl]cyclopropanecarboxylic acid,and 2-oxo-1-phenyl-imidazolidine were used as raw materials to synthesize intermediates 3a-3d,respectively. The target compounds T1-T7 were synthe?sized by chloroformylation reaction with 3a-3d. Enzyme-linked immunosorbent assay(ELISA)was used and inhibitory rate was calcu?lated to screen out the compounds with PTK inhibitory activity. Results Seven new compounds containing aroyl groups were synthe?sized and their structures were confirmed by 1H NMR. The evaluation of the seven compounds demonstrated that PTK inhibitory activi?ty of T2 and T6 were stronger than that of the lead compound. Conclusion The synthetic method is simple,and the materials are cheap and readily available. T2 and T6 show strong PTK inhibitory activity by ELISA.