Back to Search Start Over

Rapid assembly and in situ screening of bidentate inhibitors of protein tyrosine phosphatases

Rapid assembly and in situ screening of bidentate inhibitors of protein tyrosine phosphatases

Authors :
Shao Q. Yao
Rajavel Srinivasan
Mahesh Uttamchandani
Source :
Organic letters. 8(4)
Publication Year :
2006

Abstract

[reaction: see text] We have successfully designed and synthesized a small library of protein tyrosine phosphatase (PTP) inhibitors, in which the so-called "click chemistry" or Cu(I)-catalyzed 1,3-dipolar alkyne-azide coupling reaction was carried out for rapid assembly of 66 different bidentate compounds. Subsequent in situ enzymatic screening revealed a potential PTP1B inhibitor (IC(50) = 4.7 microM) which is 10-100 fold more potent than other PTPs.

Details

ISSN :
15237060
Volume :
8
Issue :
4
Database :
OpenAIRE
Journal :
Organic letters
Accession number :
edsair.doi.dedup.....20ef17f7cf6fc18b2c6d2f22d38eeac5