Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2 |
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| Authors: | Cockerill S Stubberfield C Stables J Carter M Guntrip S Smith K McKeown S Shaw R Topley P Thomsen L Affleck K Jowett A Hayes D Willson M Woollard P Spalding D |
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| Institution: | 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 |
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| 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)-dimethylpyrido3,4-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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