Details

Autor(en) / Beteiligte

• Li, Jing
• Guo, Shu Ju
• Su, Hua
• Han, Li Jun
• Shi, Da Yong

Titel

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

Ist Teil von

• Chinese chemical letters, 2008-11, Vol.19 (11), p.1290-1292

Ort / Verlag

Elsevier B.V

Erscheinungsjahr

2008

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• 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 bromophenol with significant inhibition against PTP1B which was isolated from red algae Rhodomela confervoides. Intrigued by its astonishing activity (IC 50 = 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.