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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2010-2-19
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pubmed:abstractText |
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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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1520-4804
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
25
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1862-6
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pubmed:meshHeading |
pubmed-meshheading:20095624-Animals,
pubmed-meshheading:20095624-Antineoplastic Agents,
pubmed-meshheading:20095624-Cell Line, Tumor,
pubmed-meshheading:20095624-Cell Proliferation,
pubmed-meshheading:20095624-Dioxanes,
pubmed-meshheading:20095624-Dioxolanes,
pubmed-meshheading:20095624-Drug Screening Assays, Antitumor,
pubmed-meshheading:20095624-Heterocyclic Compounds, 3-Ring,
pubmed-meshheading:20095624-Humans,
pubmed-meshheading:20095624-Mice,
pubmed-meshheading:20095624-NIH 3T3 Cells,
pubmed-meshheading:20095624-Oxepins,
pubmed-meshheading:20095624-Phosphorylation,
pubmed-meshheading:20095624-Quinazolines,
pubmed-meshheading:20095624-Receptor, Epidermal Growth Factor,
pubmed-meshheading:20095624-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Exploring epidermal growth factor receptor (EGFR) inhibitor features: the role of fused dioxygenated rings on the quinazoline scaffold.
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pubmed:affiliation |
Dipartimento di Scienze Farmaceutiche, Università di Padova, via Marzolo 5, 35131 Padova, Italy. adriana.chilin@unipd.it
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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