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Bioorg Med Chem Lett. 2008 Mar 15;18(6):1799-803. doi: 10.1016/j.bmcl.2008.02.035. Epub 2008 Feb 16.

Neutral 5-substituted 4-indazolylaminoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.

Author information

1
AstraZeneca, Centre de Recherches, Z.I.S.E. La Pompelle, B.P. 1050, 51689 Reims Cedex 2, France. bernard.barlaam2@astrazeneca.com

Abstract

We have identified a new series of C-5 substituted indazolylaminoquinazolines as potent erbB2 kinase inhibitors. The lead compound 22 showed excellent in vitro potency, good physical properties, acceptable oral pharmacokinetics in rat and dog, and low human in vitro clearance. It showed at least equivalent activity dose for dose compared to lapatinib in various erbB2- or EGFR-driven xenograft models after chronic oral administration.

PMID:
18313293
DOI:
10.1016/j.bmcl.2008.02.035
[Indexed for MEDLINE]

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