879216-95-2Relevant academic research and scientific papers
Rapid assembly and in situ screening of bidentate inhibitors of protein tyrosine phosphatases
Srinivasan, Rajavel,Uttamchandani, Mahesh,Yao, Shao Q.
, p. 713 - 716 (2006)
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.
