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.
ABSTRACT
Objective To use Ex-Rad as a lead compound to design and synthesize aryl benzyl sulfones derivatives with protein tyrosine kinase’(PTK) inhibitory activity. Methods 2-Naphthol was used as a raw material to synthesize intermediates 3a-3f. The target compounds 4a, 4d, and 5a-5f were synthesized by oxidizing 3a-3f in acetic acid with H202. Enzyme-linked immunosorbent assay’ELISA) was used and inhibition rate was calculated to screen out the compounds with PTK inhibitory activitity. Results Eight compounds containing a sulfone or sulfoxide group were synthesized and the structures were confirmed by 1H NMR. Preliminary evaluation of the 8 compounds demonstrated that the PTK inhibitory activity of 5c was much stronger than that of the lead compound. Conclusion The synthetic method is simple, and the materials are cheap and readily available. 5c shows strong PTK inhibitory activity by ELISA.
ABSTRACT
Objective To use Ex-Rad as a lead compound to design and synthesize aryl benzyl sulfones derivatives with protein tyrosine kinases(PTK) inhibitory activity. Methods 2-Naphthol was used as a raw material to synthesize intermediates 3a-3f. The target compounds 4a, 4d, and 5a-5f were synthesized by oxidizing 3a-3f in acetic acid with H2O2. Enzyme-linked immunosorbent assay(ELISA) was used and inhibition rate was calculated to screen out the compounds with PTK inhibitory activitity. Results Eight compounds containing a sulfone or sulfoxide group were synthesized and the structures were confirmed by 1H NMR. Preliminary evaluation of the 8 compounds demonstrated that the PTK inhibitory activity of 5c was much stronger than that of the lead compound. Conclusion The synthetic method is simple, and the materials are cheap and readily available. 5c shows strong PTK inhibitory activity by ELISA.