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.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / therapeutic use
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Cell Division / drug effects
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Disease Models, Animal
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ErbB Receptors / antagonists & inhibitors*
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Mice
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Mice, SCID
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Pyrimidines / therapeutic use
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Quinazolines / chemical synthesis
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Quinazolines / chemistry
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Quinazolines / pharmacology*
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Quinazolines / therapeutic use
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Receptor, ErbB-2 / antagonists & inhibitors*
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Tumor Cells, Cultured
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Xenograft Model Antitumor Assays
Substances
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4557 W
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Antineoplastic Agents
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GW 974 cpd
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Pyrimidines
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Quinazolines
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ErbB Receptors
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Receptor, ErbB-2