Author/Authors :
Alex G. Waterson، نويسنده , , Kirk L. Stevens، نويسنده , , Michael J. Reno، نويسنده , , Yue Mei Zhang، نويسنده , , Eric E. Boros، نويسنده , , Frederic Bouvier، نويسنده , , Abdullah Rastagar، نويسنده , , David E. Uehling، نويسنده , , Scott H. Dickerson، نويسنده , , Bryan Reep، نويسنده , , Octerloney B. McDonald، نويسنده , , Edgar R. Wood، نويسنده , , David W. Rusnak، نويسنده , , Krystal J. Alligood، نويسنده , , Sharon K. Rudolph، نويسنده ,
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.
Keywords :
ErbB2 , medicinal chemistry , Receptor tyrosine kinase , Kinase inhibition , EGFR