58344-59-5Relevant articles and documents
Synthesis and Biological Evaluation of 2,4,6-Trihydroxychalcone Derivatives as Novel Protein Tyrosine Phosphatase 1B Inhibitors
Sun, Liang-Peng,Gao, Li-Xin,Ma, Wei-Ping,Nan, Fa-Jun,Li, Jia,Piao, Hu-Ri
, p. 584 - 590 (2012/11/07)
A series of 2,4,6-trihydroxychalcone derivatives were synthesized and identified as reversible and competitive protein tyrosine phosphatase (PTP) 1B inhibitors with IC50 values in the micromolar range. Compound 4a had the greatest in vitro inhibition activity against PTP1B (IC50=0.27± 0.01μm) and the best selectivity (6.9-fold) for PTP1B relative to T-cell protein tyrosine phosphatases. The compounds identified herein provide a foundation on which to design specific inhibitors of PTP1B and other PTPs.
Synthesis and evaluation of antiplatelet activity of trihydroxychalcone derivatives
Zhao, Li-Ming,Jin, Hai-Shan,Sun, Liang-Peng,Piao, Hu-Ri,Quan, Zhe-Shan
, p. 5027 - 5029 (2007/10/03)
In an effort to develop potent antiplatelet agents, a series of trihydroxychalcones was synthesized and screened in vitro for their inhibitory effects on washed rabbit platelet aggregation induced by arachidonic acid (100 μM) and collagen (10 μg/ml). Of five compounds with potent inhibitory effects on arachidonic acid- and collagen-induced platelet aggregation, compound 4e was found to be the most potent. The structure-activity relationships suggested that antiplatelet activity was governed to a greater extent by the substituent on B ring of the chalcone template, and most of the active compounds had methoxy or dimethoxy groups on B ring.