179246-15-2Relevant articles and documents
QUINAZOLINE DERIVATIVES AS RAF KINASE MODULATORS AND METHODS OF USE THEREOF
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Page/Page column 176-177, (2009/10/22)
Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.
Anilinodialkoxyquinazolines: Screening epidermal growth factor receptor tyrosine kinase inhibitors for potential tumor imaging probes
VanBrocklin, Henry F.,Lim, John K.,Coffing, Stephanie L.,Hom, Darren L.,Negash, Kitaw,Ono, Michele Y.,Gilmore, Jennifer L.,Bryant, Ianthe,Riese II, David J.
, p. 7445 - 7456 (2007/10/03)
The epidermal growth factor receptor (EGFR), a long-standing drug development target, is also a desirable target for imaging. Sixteen dialkoxyquinazoline analogues, suitable for labeling with positron-emitting isotopes, have been synthesized and evaluated in a battery of in vitro assays to ascertain their chemical and biological properties. These characteristics provided the basis for the adoption of a selection schema to identify lead molecules for labeling and in vivo evaluation. A new EGFR tyrosine kinase radiometric binding assay revealed that all of the compounds possessed suitable affinity (IC50 = 0.4-51 nM) for the EGFR tyrosine kinase. All of the analogues inhibited ligand-induced EGFR tyrosine phosphorylation (IC 50 = 0.8-20 nM). The HPLC-estimated octanol/water partition coefficients ranged from 2 to 5.5. Four compounds, 4-(2′-fluoroanilino)- and 4-(3′-fluoroanilino)-6,7-diethoxyquinazoline as well as 4-(3′-chloroanilino)- and 4-(3′-bromoanilino)-6,7- dimethoxyquinazoline, possess the best combination of characteristics that warrant radioisotope labeling and further evaluation in tumor-bearing mice.
Anilinoquinazoline inhibitors of fructose 1,6-bisphosphatase bind at a novel allosteric site: Synthesis, in vitro characterization, and x-ray crystallography
Wright, Stephen W.,Carlo, Anthony A.,Carty, Maynard D.,Danley, Dennis E.,Hageman, David L.,Karam, George A.,Levy, Carolyn B.,Mansour, Mahmoud N.,Mathiowetz, Alan M.,McClure, Lester D.,Nestor, Nestor B.,McPherson, R. Kirk,Pandit, Jayvardhan,Pustilnik, Leslie R.,Schulte, Gayle K.,Soeller, Walter C.,Treadway, Judith L.,Wan, Ing-Kae,Bauer, Paul H.
, p. 3865 - 3877 (2007/10/03)
The synthesis and in vitro structure-activity relationships (SAR) of a novel series of anilinoquinazolines as allosteric inhibitors of fructose-1,6-bisphosphatase (F16Bpase) are reported. The compounds have a different SAR as inhibitors of F16Bpase than a
