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Bioorg Med Chem Lett. 2011 Jun 15;21(12):3755-8. doi: 10.1016/j.bmcl.2011.04.057. Epub 2011 Apr 23.

Design, synthesis, and evaluation of bromo-retrochalcone derivatives as protein tyrosine phosphatase 1B inhibitors.

Author information

1
College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Buk-Gu, Gwangju, Republic of Korea.

Abstract

A series of bromo-retrochalcones was designed, synthesized and evaluated as PTP1B inhibitors based on licochalcone A and E. Compounds 6, 12, 13, 14, 25, 36, 37, 39, and 41 showed potent inhibitory effects against PTP1B, and compound 37, the most potent among the series, had an IC(50) value of 1.9 μM, about two-fold better than that of the positive control, ursolic acid.

PMID:
21555221
DOI:
10.1016/j.bmcl.2011.04.057
[Indexed for MEDLINE]

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