Citation: Jing Li, Shu Ju Guo, Hua Su, Li Jun Han, Da Yong Shi. Total synthesis of bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane as potent PTP1B inhibitor[J]. Chinese Chemical Letters, ;2008, 19(11): 1290-1292. doi: 10.1016/j.cclet.2008.07.002 shu

Total synthesis of bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane as potent PTP1B inhibitor

Jing Li ^a,b, ,
Shu Ju Guo ^a,b ,
Hua Su ^a,b ,
Li Jun Han ^a ,
Da Yong Shi ^a

a Institute of Oceanology, Chinese Academy of Sciences, Qingdao 266071, China;
b Graduate School of the Chinese Academy of Sciences, Beijing 100039, China

Received Date: 21 May 2008

Fund Project: We thank to the National Center for Drug Screening (Shanghai,PR China) for supplying data on PTP1B inhibitory activities of compounds. This work was supported by the National 863 projects (Nos. 2007AA09Z410 and 2007AA091604).

Protein tyrosine phosphatase 1B (PTP1B) plays an important role as a negative regulator and has been proved to be an effective target for the treatment of type 2 diabetes mellitus.Bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane 7 was first reported as a natural bromopbenol with significant inhibition against PTP1B which was isolated from red algae Rhodomela confervoides.Intrigued by its astonishing activity (IC₅₀=2.4 μmol/L),compound 7 was synthesized with the overall yield of 24% and evaluated for its PTP1B inhibitory activity compared with natural compound.
- Bromophenol,
- Bis-(2,3-dibromo-4,5-dihydroxyphenyl)-methane,
- PTP1B inhibitor,
- Total synthesis
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