Rapid assembly and in situ screening of bidentate inhibitors of protein tyrosine phosphatases
Srinivasan, R. Uttamchandani, M. Yao, S.Q.
Srinivasan, R.
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Abstract
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 (IC50 = 4.7 μM) which is 10-100 fold more potent than other PTPs. © 2006 American Chemical Society.
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Organic Letters
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Date
2006-02-16
DOI
10.1021/ol052895w
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Article