SYNTHESIS OF NH-ACYL-ALPHA-AMINOAMIDES ON RINK RESIN - INHIBITORS OF THE HEMATOPOIETIC PROTEIN-TYROSINE-PHOSPHATASE (HEPTP)

Authors
CAO XD MORAN EJ SIEV D LIO A OHASHI C MJALLI AMM
Citation
Xd. Cao et al., SYNTHESIS OF NH-ACYL-ALPHA-AMINOAMIDES ON RINK RESIN - INHIBITORS OF THE HEMATOPOIETIC PROTEIN-TYROSINE-PHOSPHATASE (HEPTP), Bioorganic & medicinal chemistry letters, 5(24), 1995, pp. 2953-2958
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
24
Year of publication
1995
Pages
2953 - 2958
Database
ISI
SICI code
0960-894X(1995)5:24<2953:SONORR>2.0.ZU;2-J
Abstract
Cinnamic acid derivatives were prepared on Rink resin using tert-butyl -4-carboxycinnamate in a four-component Ugi condensation, Inhibition o f the hematopoietic protein tyrosine phosphatase (HePTP) by these smal l molecules is reported. An IC50 value of 3.9 mu M was determined for the most potent inhibitor discovered.