Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.

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Liu LT, Yuan TT, Liu HH, Chen SF, Wu YT

Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6373-7. Epub 2007 Aug 28.

PubMed ID

17889528 [ View in PubMed

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Abstract

A series of C-6 or C-3' alkynyl-substituted 4-anilinoquinazoline derivatives was prepared straightforwardly by a Sonogashira reaction of the corresponding bromo-substituted 4-anilinoquinazolines. Bioactive assay of these compounds for in vitro EGFR kinase inhibition demonstrated that the novel 6-hydroxypropynyl-4-anilinoquinazoline 5e was a very potent EGFR kinase inhibitor with an IC(50) of 14 nM.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Erlotinib	Epidermal growth factor receptor	IC 50 (nM)	23	N/A	N/A	Details
Gefitinib	Epidermal growth factor receptor	IC 50 (nM)	39	N/A	N/A	Details