Arylamides of hydroxylated isoquinolines as protein-tyrosine kinase inhibitors

Terrence R. Burke; Harry Ford; Nir Osherov; Alexander Levitzki; Irena Stefanova; Ivan D. Horak; Victor E. Marquez

doi:10.1016/S0960-894X(00)80473-4

Arylamides of hydroxylated isoquinolines as protein-tyrosine kinase inhibitors

Terrence R. Burke^*
, Harry Ford
, Nir Osherov
, Alexander Levitzki
, Irena Stefanova
, Ivan D. Horak
, Victor E. Marquez

^*Corresponding author for this work

Alexander Silberman Institute of Life Sciences

Research output: Contribution to journal › Article › peer-review

20 Scopus citations

Abstract

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 p56^lck and epidermal growth factor receptor (EGFR) protein-tyrosine kinases (PTKs), with the 7,8-dihydroxy substitution pattern being essential for p56^lck 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.

Original language	English
Pages (from-to)	1771-1774
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	2
Issue number	12
DOIs	https://doi.org/10.1016/S0960-894X(00)80473-4
State	Published - Dec 1992

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10.1016/S0960-894X(00)80473-4

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title = "Arylamides of hydroxylated isoquinolines as protein-tyrosine kinase inhibitors",

abstract = "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.",

author = "Burke, \{Terrence R.\} and Harry Ford and Nir Osherov and Alexander Levitzki and Irena Stefanova and Horak, \{Ivan D.\} and Marquez, \{Victor E.\}",

year = "1992",

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doi = "10.1016/S0960-894X(00)80473-4",

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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

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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

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 12

ER -

Arylamides of hydroxylated isoquinolines as protein-tyrosine kinase inhibitors

Abstract

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