Abstract
Anilinoalkynylpyrimidines were prepared and evaluated as dual EGFR/ErbB2 kinase inhibitors. A preference was found for substituted phenyl and heteroaromatic rings attached to the alkyne. In addition, the presence of a potential hydrogen bond donor appended to this ring was favored. Selected molecules in the series demonstrated some activity against human tumor cell lines.
MeSH terms
-
Alkynes / chemistry*
-
Cell Line, Tumor
-
Cell Proliferation / drug effects
-
Crystallography, X-Ray
-
Drug Screening Assays, Antitumor
-
ErbB Receptors / antagonists & inhibitors*
-
Humans
-
Models, Molecular
-
Molecular Structure
-
Pyrimidines / chemical synthesis
-
Pyrimidines / chemistry
-
Pyrimidines / pharmacology*
-
Receptor, ErbB-2 / antagonists & inhibitors*
-
Structure-Activity Relationship
Substances
-
Alkynes
-
Pyrimidines
-
ErbB Receptors
-
Receptor, ErbB-2