Synthesis of AX7593, a Quinazoline-Derived Photoaffinity Probe for EGFR

Autor:	Melissa S. Wong, Fuller, Phillip S. Leventhal, Kevin R. Shreder, Tyzoon K. Nomanbhoy
Rok vydání:	2004
Předmět:	Photoaffinity labeling Chemistry Organic Chemistry Photoaffinity Labels Biochemistry Fluorescence ErbB Receptors chemistry.chemical_compound Quinazolines Quinazoline Physical and Theoretical Chemistry Linker hormones hormone substitutes and hormone antagonists EGFR inhibitors
Zdroj:	Organic Letters. 6:3715-3718
ISSN:	1523-7052 1523-7060
Popis:	[structure: see text] The synthesis of a photoaffinity probe for EGFR is described. O-Alkylation of 4-(meta-azidoanilino)-6-methoxy-7-hydroxy-quinazoline with a protected tetraethyleneglycol linker followed by the attachment of tetramethylrhodamine yielded the fluorescent probe AX7593. Photoaffinity labeling of EGFR by AX7593 (K(b) = 280 nM) was shown to have an efficiency of 34% and to be competitive with the EGFR inhibitors PP2 and AG1478.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3977075c421407a793e34a5fc5052da https://doi.org/10.1021/ol048656a Zobrazit plný text záznamu