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

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

  • Bioorg Med Chem Lett. 2001 Jun 4;11(11):1401-5. doi: 10.1016/s0960-894x(01)00219-0.
S Cockerill 1,  C Stubberfield,  J Stables,  M Carter,  S Guntrip,  K Smith,  S McKeown,  R Shaw,  P Topley,  L Thomsen,  K Affleck,  A Jowett,  D Hayes,  M Willson,  P Woollard,  D Spalding
Affiliations

Affiliation

  • 1 Enzyme Chemistry 1, Oncology Unit, Enzyme Pharmacology, Research Biomet. Glaxo Wellcome Medicines Research Centre, Gunnels Wood Road, Hertfordshire SG1 2NY, Stevenage, UK. [email protected]
PMID: 11378364 DOI: 10.1016/s0960-894x(01)00219-0
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.

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