Impact of aryloxy-linked quinazolines: a novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors.

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Garofalo A, Goossens L, Six P, Lemoine A, Ravez S, Farce A, Depreux P

Impact of aryloxy-linked quinazolines: a novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):2106-12. doi: 10.1016/j.bmcl.2011.01.137. Epub 2011 Feb 3.

PubMed ID

21353546 [ View in PubMed

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Abstract

Three series of 6,7-dimethoxyquinazoline derivatives substituted in the 4-position by aniline, N-methylaniline and aryloxy entities, targeting EGFR and VEGFR-2 tyrosine kinases, were designed and synthesized. Pharmacological activities of these compounds have been evaluated for their enzymatic inhibition of VEGFR-2 and EGFR and for their antiproliferative activities on various cancer cell lines. We have studied the impact of the variation in the 4-position substitution of the quinazoline core. Substitution by aryloxy groups led to new compounds which are selective inhibitors of VEGFR-2 enzyme with IC(50) values in the nanomolar range in vitro.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Vandetanib	Epidermal growth factor receptor	IC 50 (nM)	800	N/A	N/A	Details
Vandetanib	Epidermal growth factor receptor	IC 50 (nM)	500	N/A	N/A	Details