206755-40-0Relevant articles and documents
Synthesis and biological evaluation of geniposide derivatives as potent and selective PTPlB inhibitors
Lei, Shuwen,Zhang, Dongdong,Qi, Yunyue,Chowdhury, Sharmin Reza,Sun, Ran,Wang, Juntao,Du, Yi,Fu, Lei,Jiang, Faqin
, (2020)
Herein a series of Geniposide derivatives were designed, synthesized and evaluated as protein tyrosine phosphatase 1B (PTPlB) inhibitors. Most of these compounds exhibited potent in vitro PTP1B inhibitory activities, the representative 7a and 17f were found to be the most potent inhibitors against the enzyme with IC50 values of 0.35 and 0.41 μM, respectively. More importantly, they showcased 4 to10-fold selectivity over SHP2 and 3-fold over TCPTP. Further biological activity studies revealed that compounds 7a, 17b and 17f could effectively enhance insulin-stimulated glucose uptake with no significant cytotoxicity. Subsequent molecular docking and structural activity relationship analyses demonstrated that the glucose scaffold, benzylated glycosyl groups, and arylethenesulfonic acid ester significantly impact on the activity and selectivity.
Genipin derivatives and their preparation method and use
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Paragraph 0126; 0162-0164, (2018/03/01)
The invention provides genipin derivatives and their preparation method and use and specifically discloses genipin derivatives having novel structures shown in the formula I. The groups are defined in the specification. The invention also discloses a preparation method of the compounds and use of the compounds as protein tyrosine phosphatase 1B (PTP1B) inhibitors. The compounds produce good anti-diabetic effects and have an application value in preparation of drugs for treating type II diabetes.
