Exploring epidermal growth factor receptor (EGFR) inhibitor features: the role of fused dioxygenated rings on the quinazoline scaffold.
作者： Adriana Chilin , Maria Teresa Conconi , Giovanni Marzaro , Adriano Guiotto , Luca Urbani
DOI: 10.1021/JM901338G
关键词:
摘要: A number of dioxolane, dioxane, and dioxepine quinazoline derivatives have been synthetized evaluated as EGFR inhibitors. Their cytotoxic activity has tested against two cell lines overexpressing not expressing EGFR. Most were able to counteract EGF-induced phosphorylation, their potency was comparable the reference compound PD153035. The size fused dioxygenated ring crucial for biological activity, dioxane being most promising class this series.
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