113283-93-5Relevant academic research and scientific papers
Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting the αvβ3 Integrin/VEGFR2 Couple and Impairing Tumor-Associated Angiogenesis
Sartori, Andrea,Portioli, Elisabetta,Battistini, Lucia,Calorini, Lido,Pupi, Alberto,Vacondio, Federica,Arosio, Daniela,Bianchini, Francesca,Zanardi, Franca
, p. 248 - 262 (2017)
On the basis of a previously discovered anti-αVβ3 integrin peptidomimetic (c(AmpRGD)) and the clinically approved antiangiogenic kinase inhibitor sunitinib, three novel dual conjugates were synthesized (compounds 1-3), featuring the covalent and robust linkage between these two active modules. In all conjugates, the ligand binding competence toward αVβ3 (using both isolated receptors and αVβ3-overexpressing endothelial progenitor EP cells) and the kinase inhibitory activity (toward both isolated kinases and EPCs) remained almost untouched and comparable to the activity of the single active units. Compounds 1-3 showed interesting antiangiogenesis properties in an in vitro tubulogenic assay; furthermore, dimeric-RGD conjugate 3 strongly inhibited in vivo angiogenesis in Matrigel plug assays in FVB mice. These results offer proof-of-concept of how the covalent conjugation of two angiogenesis-related small modules may result in novel and stable molecules, which impair tumor-related angiogenesis with equal or even superior ability as compared to the single modules or their simple combinations.
Selective mono-BOC protection of diamines
Lee, Dae Woo,Ha, Hyun-Joon,Lee, Won Koo
, p. 737 - 742 (2007)
A facile route for mono-BOC protection of symmetrical and unsymmetrical diamines was developed by sequential additions of 1 mol of HCl and 1 mol of (BOC)2O followed by neutralization. Copyright Taylor & Francis Group, LLC.
Polymer-des-ethyl sunitinib conjugates
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Page/Page column 63-64, (2019/03/14)
The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form.
COMPOUNDS AND METHODS
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Page/Page column 40; 45, (2013/03/26)
Disclosed are compounds having formula I, wherein X1, X2, X3, R1, R2, R3, R4, R5, Y, A, Z, L, m and n are as defined herein, and methods of making and using the same.
THERAPEUTIC AGENT FOR CEREBRAL INFARCTION
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, (2012/08/08)
The invention provides a therapeutic drug for ischemic stroke. The therapeutic drug has the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof, as an active ingredient.
AMIDOETHYL ALKYLAMINO OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 31, (2009/03/07)
The present invention is directed to amidoethylamine compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Bifunctional energy-reversible acyl-compositions
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, (2008/06/13)
Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed. In preferred aspects, examples of such compositions include:
