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

Authors :
Ballard P
Barlaam BC
Bradbury RH
Dishington A
Hennequin LF
Hickinson DM
Hollingsworth IM
Kettle JG
Klinowska T
Ogilvie DJ
Pearson SE
Scott JS
Suleman A
Whittaker R
Williams EJ
Wood R
Wright L
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2007 Nov 15; Vol. 17 (22), pp. 6326-9. Date of Electronic Publication: 2007 Sep 02.
Publication Year :
2007

Abstract

Neutral 5-substituted 4-anilinoquinazolines addressed high in vivo clearance and phospholipidosis associated with previous basic compounds. A representative compound 8a inhibited tumor growth in a mouse xenograft model when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole (ABT), and data are consistent with pharmacology primarily reflecting inhibition of erbB2 receptor tyrosine kinase.

Details

Language :
English
ISSN :
0960-894X
Volume :
17
Issue :
22
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
17869514
Full Text :
https://doi.org/10.1016/j.bmcl.2007.08.073