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

Rajavel Srinivasan, Mahesh Uttamchandani, Shao Q Yao

Index: Org. Lett. 8(4) , 713-6, (2006)

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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.