Synthesis and PTP1B inhibition of novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes.
作者信息
Wrobel J, Li Z, Sredy J, Sawicki D R, Seestaller L, Sullivan D
机构信息
Wyeth-Ayerst Research, Inc., Princeton, NJ 08543-8000, USA.
出版信息
Bioorg Med Chem Lett. 2000 Jul 17;10(14):1535-8. doi: 10.1016/s0960-894x(00)00278-x.
Abstract
Novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes were designed, synthesized, and evaluated as inhibitors of the protein tyrosine phosphatase, PTP1B. Compounds 3 (IC50 = 284 nM) and 4 (IC50 = 74 nM), showed nanomolar potency against PTP1B (TRDI(P)YETD(P)Y(P)YRK as substrate). Compound 4 also lowered insulin in the diabetic ob/ob mouse at a dose of 10 mg/kg/day, p.o.
摘要
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