TY - JOUR
T1 - Arylamides of hydroxylated isoquinolines as protein-tyrosine kinase inhibitors
AU - Burke, Terrence R.
AU - Ford, Harry
AU - Osherov, Nir
AU - Levitzki, Alexander
AU - Stefanova, Irena
AU - Horak, Ivan D.
AU - Marquez, Victor E.
PY - 1992/12
Y1 - 1992/12
N2 - Aryl-substituted amides of isomeric 6,7- and 7,8-dihydroxyisoquinoline-3-carboxamides (2 and 3)_ were prepared. Divergent structural requirements were observed for inhibiting p56lck and epidermal growth factor receptor (EGFR) protein-tyrosine kinases (PTKs), with the 7,8-dihydroxy substitution pattern being essential for p56lck activity, and the arylamide being required for EGFR potency. The work presents a useful approach toward the design of inhibitors which can discriminate between different PTKs.
AB - Aryl-substituted amides of isomeric 6,7- and 7,8-dihydroxyisoquinoline-3-carboxamides (2 and 3)_ were prepared. Divergent structural requirements were observed for inhibiting p56lck and epidermal growth factor receptor (EGFR) protein-tyrosine kinases (PTKs), with the 7,8-dihydroxy substitution pattern being essential for p56lck activity, and the arylamide being required for EGFR potency. The work presents a useful approach toward the design of inhibitors which can discriminate between different PTKs.
UR - https://www.scopus.com/pages/publications/0026621832
U2 - 10.1016/S0960-894X(00)80473-4
DO - 10.1016/S0960-894X(00)80473-4
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AN - SCOPUS:0026621832
SN - 0960-894X
VL - 2
SP - 1771
EP - 1774
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 12
ER -
