Structural influences of styryl-based inhibitors on epidermal growth factor receptor and p56lck tyrosine-specific protein kinases.

Bioorganic & Medicinal Chemistry Letters
1991.0

Abstract

A structure activity study was conducted on two important members of the styryl class of tyrosine-specific protein kinase inhibitors to examine relative roles which the aryl rings and vinyl side chains play in their inhibitory activity. The ability of four analogs (1a-d) to inhibit autophosphorylation of epidermal growth factor receptor (EGFR) and p56lck tyrosine kinases was examined, with results showing that both the pattern of aromatic hydroxylation and the type of side chain functionality can greatly influence both selectivity and potency.

Knowledge Graph

Similar Paper

Structural influences of styryl-based inhibitors on epidermal growth factor receptor and p56lck tyrosine-specific protein kinases.
Bioorganic & Medicinal Chemistry Letters 1991.0
Structure-Activity Relationships in a Series of 5-[(2,5-Dihydroxybenzyl)amino]salicylate Inhibitors of EGF-Receptor-Associated Tyrosine Kinase: Importance of Additional Hydrophobic Aromatic Interactions
Journal of Medicinal Chemistry 1994.0
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors
Journal of Medicinal Chemistry 1989.0
Hydroxylated 2-(5'-salicyl)naphthalenes as protein-tyrosine kinase inhibitors
Journal of Medicinal Chemistry 1993.0
Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor-associated tyrosine kinase activity
Journal of Medicinal Chemistry 1993.0
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: Synthesis and structure–activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 2006.0
Sulfonylbenzoyl-nitrostyrenes: Potential bisubstrate type inhibitors of the EGF-receptor tyrosine protein kinase
Journal of Medicinal Chemistry 1991.0
Inhibitors of epidermal growth factor receptor tyrosine kinase: Optimisation of potency and in vivo pharmacokinetics
Bioorganic & Medicinal Chemistry Letters 2006.0
Synthesis and biological activity of 5-[(2,5-dihydroxybenzyl)amino]salicylic acid analogs as inhibitors of EGF receptor-associated protein tyrosine kinase
Bioorganic & Medicinal Chemistry Letters 1997.0
Synthesis and Biological Evaluations of 3-Substituted Indolin-2-ones:  A Novel Class of Tyrosine Kinase Inhibitors That Exhibit Selectivity toward Particular Receptor Tyrosine Kinases
Journal of Medicinal Chemistry 1998.0