Tyrphostins IV--highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines

A Gazit; J Chen; H App; G McMahon; P Hirth; I Chen; A Levitzki

doi:10.1016/0968-0896(96)00107-1

Tyrphostins IV--highly potent inhibitors of EGF receptor kinase. Structure-activity relationship study of 4-anilidoquinazolines

Bioorg Med Chem. 1996 Aug;4(8):1203-7. doi: 10.1016/0968-0896(96)00107-1.

Authors

A Gazit¹, J Chen, H App, G McMahon, P Hirth, I Chen, A Levitzki

Affiliation

¹ Department of Organic Chemistry, Alexander Silverman Institute of Life Sciences, Hebrew University of Jerusalem, Israel.

PMID: 8879541
DOI: 10.1016/0968-0896(96)00107-1

Abstract

Potent 4-anilido-substituted quinazolines which potently inhibit epidermal growth factor receptor (EGFR) kinase were prepared. Structure-activity relationship studies reveal high sensitivity to substitution at the aniline ring.

MeSH terms

Aniline Compounds / chemistry*
ErbB Receptors / antagonists & inhibitors*
Phosphorylation
Protein Kinase C / antagonists & inhibitors
Quinazolines / chemistry*
Staurosporine / pharmacology
Structure-Activity Relationship

Substances

Aniline Compounds
Quinazolines
ErbB Receptors
Protein Kinase C
Staurosporine
aniline