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ID: ALA1147619

Journal: Bioorg Med Chem Lett

Title: Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles.

Authors: Wissner A, Hamann PR, Nilakantan R, Greenberger LM, Ye F, Rapuano TA, Loganzo F.

Abstract: The syntheses and EGFR kinase inhibitory activity of a series of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles are described. Both reversible and irreversible binding inhibitors were prepared. These series were compared with each other and with the corresponding 4-anilinoquinoline-3-carbonitriles. Compounds having a 1,7-naphthyridine core structure can retain high potency while those with a 1,8-naphthyridine core are significantly less active. These results are consistent with molecular modeling observations.

CiteXplore: 15006373

DOI: 10.1016/j.bmcl.2004.01.034