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Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5.

Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.

Author information

1
Enzyme Chemistry 1, Oncology Unit, Enzyme Pharmacology, Research Biomet. Glaxo Wellcome Medicines Research Centre, Gunnels Wood Road, Hertfordshire SG1 2NY, Stevenage, UK. scockerill@arrowt.co.uk

Abstract

Described herein is the design and synthesis of indazolylaminopyridopyrimidines and quinazolines as inhibitors of the class 1 tyrosine kinase receptor family. Data is presented for N(4)-(1-benzyl-1H-indazol-5-yl)-N(6),N(6)-dimethylpyrido[3,4-d]pyrimidine-4,6-diamine 3B. This compound inhibited EGFr and c-erbB-2 enzymes selectively over other kinases. It inhibited the proliferation of a range of tumour cell lines in vitro and the growth of BT474 xenografts in SCID mice.

PMID:
11378364
DOI:
10.1016/s0960-894x(01)00219-0
[Indexed for MEDLINE]

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