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Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
- 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.
- Subjects :
- Administration, Oral
Aniline Compounds chemistry
Animals
Antineoplastic Agents pharmacokinetics
Antineoplastic Combined Chemotherapy Protocols
Cell Proliferation drug effects
Dogs
Drug Synergism
Mice
Molecular Structure
Quinazolines pharmacokinetics
Rats
Triazoles pharmacology
Xenograft Model Antitumor Assays
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Neoplasms drug therapy
Quinazolines chemistry
Quinazolines pharmacology
Receptor, ErbB-2 antagonists & inhibitors
Subjects
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