2. Academic Validation
  3. Exploring epidermal growth factor receptor (EGFR) inhibitor features: the role of fused dioxygenated rings on the quinazoline scaffold

Exploring epidermal growth factor receptor (EGFR) inhibitor features: the role of fused dioxygenated rings on the quinazoline scaffold

  • J Med Chem. 2010 Feb 25;53(4):1862-6. doi: 10.1021/jm901338g.
Adriana Chilin 1,  Maria Teresa Conconi,  Giovanni Marzaro,  Adriano Guiotto,  Luca Urbani,  Francesca Tonus,  Pierpaolo Parnigotto
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università di Padova, via Marzolo 5, 35131 Padova, Italy. adriana.chilin@unipd.it
PMID: 20095624 DOI: 10.1021/jm901338g
Abstract

A number of dioxolane, dioxane, and dioxepine quinazoline derivatives have been synthetized and evaluated as EGFR inhibitors. Their cytotoxic activity has been tested against two cell lines overexpressing and not expressing EGFR. Most derivatives were able to counteract EGF-induced EGFR phosphorylation, and their potency was comparable to the reference compound PD153035. The size of the fused dioxygenated ring was crucial for the biological activity, the dioxane derivatives being the most promising class of this series.

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