264254-52-6Relevant academic research and scientific papers
Synthesis and PTP1B inhibition of novel 4-aryl-1-oxa-9-thiacyclopenta[b]fluorenes
Wrobel, Jay,Li, Zenan,Sredy, Janet,Sawicki, Diane R.,Seestaller, Laura,Sullivan, Donald
, p. 1535 - 1538 (2007/10/03)
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)YRK as substrate). Compound 4 also lowered insulin in the diabetic ob/ob mouse at a dose of 10 mg/kg/day, po. (C) 2000 Elsevier Science Ltd. All rights reserved.
