5950-16-3Relevant academic research and scientific papers
Fluorescent non-peptidic RGD mimetics with high selectivity for αvβ3 vs αiIbβ3 integrin receptor: Novel probes for in vivo optical imaging
Alsibai, Wael,Hahnenkamp, Anke,Eisenbl?tter, Michel,Riemann, Burkhard,Sch?fers, Michael,Bremer, Christoph,Haufe, Günter,H?ltke, Carsten
, p. 9971 - 9982 (2015/02/02)
Integrins are heterodimeric transmembrane protein receptors consisting of different α and β subunits. αvβ3 integrins are overexpressed on many tumor cells and tumor-associated angiogenic vessels, whereas αIIbβ3 is a receptor for, e.g., fibrinogen and mediates platelet aggregation. In this study, a near-infrared fluorescent imaging probe has been designed and synthesized by conjugating fluorescent dyes to a non-peptidic, pharmacophore-based ligand, based on a molecular modeling design approach. Affinity values were determined, and in vitro cell binding assays and preliminary in vivo xenograft studies in nude mice were performed to evaluate target binding. Competition assays revealed excellent binding and selectivity to αvβ3 compared to that for αIIbβ3. In vitro, the probe showed high target binding on αvβ3-positive M-21 cells and negligible binding to αvβ3-negative MCF-7 cells. In vivo, the tracer is able to image target expression in U-87 xenografts with a maximum signal-to-noise ratio (SNR) of 2.5:1 at 24 h after injection.
Novel Compounds Active as Muscarinic Receptor Antagonists
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Page/Page column 13-14, (2009/04/24)
The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical compositions containing them.
Novel and potent anti-malarial agents
Brinner, Kristin M,Mi Kim, Jin,Habashita, Hiromu,Gluzman, Ilya Y,Goldberg, Daniel E,Ellman, Jonathan A
, p. 3649 - 3661 (2007/10/03)
Readily accessible, novel, and potent anti-malarial compounds have been developed. Optimization of the initial lead structure resulted in derivatives with IC50 values from 7 to 35 nM against chloroquine-sensitive and 70-350 nM against chloroquine-resistant strains of Plasmodium falciparum.
