103143-17-5Relevant articles and documents
Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP)
Antoni, Frauke,Bauer, Stefanie,Bause, Manuel,Bernhardt, Günther,Buschauer, Armin,Jackson, Scott M.,K?nig, Burkhard,Locher, Kaspar P.,Manolaridis, Ioannis,Scholler, Matthias,Stark, Simone A.
supporting information, (2020/02/26)
Tariquidar derivatives have been described as potent and selective ABCG2 inhibitors. However, their susceptibility to hydrolysis limits their applicability. The current study comprises the synthesis and characterization of novel tariquidar-related inhibit
Substituted indolines which inhibit receptor tyrosine kinases
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Page column 43, (2008/06/13)
Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
2-(aminobenzyl)-1,2,3,4-tetrahydroisoquinolines: A new class of α2-adrenergic receptor antagonists
Stambach,Kanmacher,Jung,Schott,Heitz,Stoclet
, p. 427 - 432 (2007/10/02)
A new class of α2-adrenergic receptor antagonists, the 2-(aminobenzyl)-1,2,3,4-tetrahydroisoquinolines 4 and their derivatives, is described. Two synthetic routes are reported. An investigation of the structure-activity relationships including various substitutions of the isoquinoline moiety and the benzyl group is discussed. The affinity and selectivity for both α1- and α2-adrenoceptors was defined by studying the displacement of [3H]-prazosin (α1-sites) and [3H]-yohimbine (α2-sites) from rat brain membranes. The 2-(2-amino-3,4-dimethoxybenzyl)-6-methoxy-1,2,3,4- tetrahydroisoquinoline 4a presented affinity and selectivity close to yohimbine. In functional experiments the α-adrenoceptor blocking properties of 4a have been evaluated on isolated rat aorta and on the twitch responses of the isolated rat vas deferens.