Journal
ARCHIV DER PHARMAZIE
Volume 345, Issue 6, Pages 444-453Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201100373
Keywords
Bromophenol; Protein tyrosine phosphatase 1B inhibitor; Structure-activity relationship; Type 2 diabetes mellitus
Funding
- National Major Research Program of China The Creation for Significant Innovative Drugs [2009ZX09103-148]
- National Natural Science Foundation of Shandong [BS2009YY011]
- National Natural Science Foundation of Qingdao [10-3-4-8-2-JCH]
- Program of Qingdao Shinan District [2009-HY-2-14]
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3-Bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (BDB) is a bromophenol purified from the marine red alga Rhodomela confervoides and exhibits potent protein tyrosine phosphatase 1B (PTP1B) inhibition (IC50?=?1.7?mu mol/L). In an effort to improve the PTP1B inhibitory activity, a series of derivatives were designed, synthesized, and evaluated in vitro. The preliminary structureactivity relationship indicated that the tricyclic scaffold and multi-bromine atoms (four to five) attached to the aryl rings are important for PTP1B inhibition. Among these, compound 26 exhibited remarkable inhibitory activity against PTP1B with an IC50 of 0.89 mu mol/L, which was approximately two-fold more potent than the initial lead compound BDB.
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