388622-47-7Relevant articles and documents
Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: Design, synthesis, and evaluation
Harmange, Jean-Christophe,Weiss, Matthew M.,Germain, Julie,Polverino, Anthony J.,Borg, George,Bready, James,Chen, Danlin,Choquette, Deborah,Coxon, Angela,DeMelfi, Tom,DiPietro, Lucian,Doerr, Nicholas,Estrada, Juan,Flynn, Julie,Graceffa, Russell F.,Harriman, Shawn P.,Kaufman, Stephen,La, Daniel S.,Long, Alexander,Martin, Matthew W.,Neervannan, Sesha,Patel, Vinod F.,Potashman, Michele,Regal, Kelly,Roveto, Phillip M.,Schrag, Michael L.,Starnes, Charlie,Tasker, Andrew,Teffera, Yohannes,Wang, Ling,White, Ryan D.,Whittington, Douglas A.,Zanon, Roger
, p. 1649 - 1667 (2008)
A series of naphthyl-based compounds were synthesized as potential inhibitors of vascular endothelial growth factor (VEGF) receptors. Investigations of structure-activity relationships led to the identification of a series of naphthamides that are potent inhibitors of the VEGF receptor tyrosine kinase family. Numerous analogues demonstrated low nanomolar inhibition of VEGF-dependent human umbilical vein endothelial cell (HUVEC) proliferation, and of these several compounds possessed favorable pharmacokinetic (PK) profiles. In particular, compound 48 demonstrated significant antitumor efficacy against established HT29 human colon adenocarcinoma xenografts implanted in athymic mice. A full account of the preparation, structure-activity relationships, pharmacokinetic properties, and pharmacology of analogues within this series is presented.
Aniline pyrimidines, its preparation method and medical use (by machine translation)
-
, (2018/03/01)
The invention relates to: an aniline pyrimidine compound represented as the formula (I), a medicinal salt thereof, a prodrug thereof, and a hydrate or solvate thereof and also relates to: the preparation method of the compound, a medicine composition comp
NAPHTHYLAMIDE COMPOUND, PREPARATION METHOD AND USE THEREOF
-
, (2017/01/09)
The present invention relates to a naphthylamide compound of the structure as represented by formula (I), medicinal salts, prodrugs and hydrates or solvates thereof, and also relates to a method of preparing the compounds, pharmaceutical compositions comp
FLUORESCENT CALCIUM INDICATORS THAT ARE RATIOMETRIC AND EMIT IN THE RED SPECTRUM
-
Page/Page column 11; 12, (2011/05/05)
A new generation of fluorescent ion indicators for measuring cytosolic concentrations of calcium. These new indicators emit in the red portion of the visible spectrum and are ratiometric. The ratiometry consists of shifting in the emission upon binding ca
Synthesis and photophysical properties of new fluorinated benzo[c]xanthene dyes as intracellular pH indicators
Liu, Jixiang,Diwu, Zhenjun,Leung, Wai-Yee
, p. 2903 - 2905 (2007/10/03)
Two new fluorinated benzo[c]xanthene dyes were synthesized by reaction of fluorinated 1,6-dihydroxynaphthalenes with 2,4- (and 2,5)-dicarboxy-3′-dimethylamino-2′-hydroxybenzophenone. The two critical fluorinated 1,6-dihydroxynaphthalene intermediates were prepared via a regioselective route. The fluorinated benzo[c]xanthene dyes exhibit desired lower pKa values (6.4 and 7.2, respectively) than their parent compound (pKa = 7.5) while the pH-dependent dual-emission characteristics are well retained. Their cell-permeable esters have been prepared for intracellular applications.