Synthesis and evaluation of multisubstrate inhibitors of an oncogene-encoded tyrosine-specific protein kinase. 1

CH Kruse, KG Holden, ML Pritchard…

Index: Kruse, Carolyn H.; Holden, Kenneth G.; Pritchard, M. Lynn; Feild, John A.; Rieman, David J.; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 9 p. 1762 - 1767

Full Text: HTML

Citation Number: 28

Abstract

The synthesis and testing of potential multisubstrate inhibitors of tyrosine-specific protein kinases are described. One of the substrates, ATP, was mimicked by the known kinase inhibitor 5'-[4-(fluorosulfonyl) benzoyl] adenosine, which was covalently linked via the sulfonyl moiety to tyrosine mimics. The resulting multisubstrate inhibitors were tested for their ability to inhibit the transfer of phosphate from ATP to a protein acceptor by~ 60"-"~', the ...