Journal
ORGANIC LETTERS
Volume 8, Issue 4, Pages 713-716Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol052895w
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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 mu M) which is 10-100 fold more potent than other PTPs.
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