Synthesis of Nh-acyl-α-aminoamides on rink resin: Inhibitors of the hematopoietic protein tyrosine phosphatase (HePTP)

Cinnamic acid derivatives were prepared on Rink resin using tert-butyl-4-carboxycinnamate in a four-component Ugi condensation. Inhibition of the hematopoietic protein tyrosine phosphatase (HePTP) by these small molecules is reported. An IC 50 value of 3.9 μM was determined for the most potent inhib...

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Published inBioorganic & medicinal chemistry letters Vol. 5; no. 24; pp. 2953 - 2958
Main Authors Xiaodong Cao, Moran, Edmund J., Siev, Daniel, Lio, Anna, Ohashi, Cara, Mjalli, Adnan M.M.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 21.12.1995
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Summary:Cinnamic acid derivatives were prepared on Rink resin using tert-butyl-4-carboxycinnamate in a four-component Ugi condensation. Inhibition of the hematopoietic protein tyrosine phosphatase (HePTP) by these small molecules is reported. An IC 50 value of 3.9 μM was determined for the most potent inhibitor discovered. Cinnamic acid derivatives were prepared on Rink resin using tert-butyl-4-carboxycinnamate in a four-component Ugi condensation. Inhibition of the hematopoietic protein tyrosine phosphatase (HePTP) by these small molecules is reported. An IC 50 value of 3.9 μM was determined for the most potent inhibitor discovered.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(95)00533-6