Novel heterocyclic ring-fused oleanolic acid derivatives as osteoclast inhibitors for osteoporosis
Osteoporosis is a major public health problem in our aging society. In the present study, a series of novel oleanolic acid (OA) derivatives were synthesized via modifications in the A-ring and C-28 position of OA, and their anti-bone resorption activities
Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B
A series of maslinic acid derivatives have been synthesized by introducing various fused heterocyclic rings at C-2 and C-3 positions. Their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Most of the compounds exhibited a dramatic increase in inhibitory potency and selectivity, the two most potent PTP1B inhibitors 20 (IC50 = 0.61 μM) and 29 (IC50 = 0.64 μM) showed about 10-fold more potent than lead compound maslinic acid. More importantly, 29 possesses the best selectivity of 6.9-fold for PTP1B over TCPTP.
Qiu, Wen-Wei,Shen, Qiang,Yang, Fan,Wang, Bo,Zou, Hui,Li, Jing-Ya,Li, Jia,Tang, Jie
scheme or table
p. 6618 - 6622
(2010/06/12)
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