Synthesis and protein tyrosine kinases inhibitory activity of aroyl derivatives
10.13220/j.cnki.jipr.2016.03.013
- Author:
Yu-Lan TANG
1
Author Information
1. Anhui Medical University
- Publication Type:Journal Article
- Keywords:
Aroyl group;
Design and synthesis;
Protein tyrosine kinases inhibitor
- From:
Journal of International Pharmaceutical Research
2016;43(3):471-475
- CountryChina
- Language:Chinese
-
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.
