Design, synthesis and anti-inflammatory evaluation of CDDO-Me ester prodrugs / 中国药科大学学报
Journal of China Pharmaceutical University
; (6): 661-665, 2016.
Article
em Zh
| WPRIM
| ID: wpr-811878
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WPRO
ABSTRACT
@#In order to search for new anti-inflammatory agents with strong activity and less toxicity relative to CDDO-Me, the ester prodrugs 2-8 of CDDO-Me were synthesized by treatment of oleanolic acid(OA)with DMF/K2CO3 to generate 1, followed by esterification of 1 with various aliphatic and aromatic carboxylic acids, respectively. All the target compounds showed strong inhibitory effects on LPS-induced NO production in RAW 264. 7 cells. Among them, compounds 2 and 7 possessed the most potent inhibitory effects with IC50=(2. 34±0. 67)and(3. 83±0. 97)nmol/L, respectively. Moreover, MTT assay indicated that all the target compounds(2-8)displayed much weaker anti-proliferative activity against RAW 264. 7 cell lines than CDDO-Me, suggesting that they may be less toxic than CDDO-Me.
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Base de dados:
WPRIM
Idioma:
Zh
Revista:
Journal of China Pharmaceutical University
Ano de publicação:
2016
Tipo de documento:
Article