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Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors.

Waterson AG, Petrov KG, Hornberger KR, Hubbard RD, Sammond DM, Smith SC, Dickson HD, Caferro TR, Hinkle KW, Stevens KL, Dickerson SH, Rusnak DW, Spehar GM, Wood ER, Griffin RJ, Uehling DE
Bioorg Med Chem Lett. 2009 19 (5): 1332-6

PMID: 19208477 · DOI:10.1016/j.bmcl.2009.01.080

Aniline 'headgroups' were synthesized and incorporated into an alkynyl thienopyrimidine series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein binding was reduced and oral exposure was found to be somewhat improved relative to compounds containing the reference aniline.

MeSH Terms (13)

Administration, Oral Aniline Compounds Animals Cell Line, Tumor Cell Proliferation Drug Evaluation, Preclinical ErbB Receptors Growth Inhibitors Humans Mice Protein Kinase Inhibitors Pyrimidines Receptor, ErbB-2

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