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against PTP1B and good selectivity over other PTPs (TCPTP, SHP-
1, SHP-2 and LAR). The 14b as a competitive inhibitor of PTP1B
was confirmed by an enzymatic kinetic study. Moreover, the good
activity of 14b and a 14-fold selectivity over TCPTP were well sup-
ported by the binding interactions with PTP1B and TCPTP respec-
tively on a docking model. This Letter showed an effective way
for discovering specific potentinhibitors of PTP1B by modifying
naturally steroid compounds. Currently we are in the process of
further SAR research and evaluation in cell models, which will be
reported in due time.
Acknowledgments
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This work was supported by National Nature Science Founda-
tion of China(81125023) and National Science and Technology Ma-
jor Projects for Major New Drugs Innovation and Development
(2012ZX09304011), Shanghai Science and Technology council
(No. 10142200802 and 11DZ2292200). We also thank ‘Lab of Or-
ganic Functional Molecules, THE SINO-FRENCH INSTITUTE OF ECNU’
for supports.
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