103796-34-5Relevant articles and documents
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 (2005)
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.
Lipoprotein Signal Peptidase Inhibitors with Antibiotic Properties Identified through Design of a Robust In Vitro HT Platform
Kitamura, Seiya,Owensby, Anna,Wall, Daniel,Wolan, Dennis W.
, p. 301 - 12,308 (2018)
As resistance to antibiotics increases, the exploration of new targets and strategies to combat pathogenic bacteria becomes more urgent. Ideal protein targets are required for viability across many species, are unique to prokaryotes to limit effects on th
BENZAMIDE INHIBITORS OF BACTERICAL LIPOPROTEIN SIGNAL PEPTIDASE
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Page/Page column 26, (2019/01/21)
Increasing resistance to antibiotics necessitates discovery of new targets and strategies to combat bacteria. Ideal protein targets are required for viability across many species, are unique to prokaryotes to limit effects on the host and have robust assa
Quinazoline derivatives and therapeutic use thereof
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Page/Page column 18, (2008/06/13)
Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperproliferative disorders are also described.
