Synthesis and biological evaluation of oleanolic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B
A series of oleanolic acid (OA) derivatives have been synthesized and their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Some compounds with five-membered heterocyclic ring-fused at C-2, C-3 positions showed a dramatic increase in in
Li, Hui,Zou, Hui,Gao, Lixin,Liu, Ting,Yang, Fan,Li, Jingya,Li, Jia,Qiu, Wen-Wei,Tang, Jie
p. 1117 - 1139
(2012/08/07)
Pentacyclic triterpenes. Part 3: Synthesis and biological evaluation of oleanolic acid derivatives as novel inhibitors of glycogen phosphorylase
Oleanolic acid and its synthetic derivatives have been identified as novel inhibitors of glycogen phosphorylase. Within this series of compounds, 4 (IC50 = 3.3 μM) is the most potent GPa inhibitor. Preliminary structure-activity relationships of the oleanolic acid derivatives are discussed.