Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, Product Details of 142-45-0, 142-45-0, Name is Acetylenedicarboxylic Acid, SMILES is O=C(C#CC(O)=O)O, belongs to quinuclidines compound. In a document, author is Venkateswaran, Amudhan, introduce the new discover.
Antiangiogenic properties of substituted (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ol/one analogs and their derivatives
In the past half century research efforts have defined a critical role for angiogenesis in tumor growth and metastasis. We previously reported that inhibition of a novel target, ENOX1, by a (Z)-2-benzylindol-3-ylmethylene) quinuclidin-3-ol, suppressed tumor angiogenesis. The present study was undertaken in order to establish structure-activity relationships for quinuclidine analogs. The angiogenesis inhibiting activity of a series of substituted (Z)-(+/-)-2-(N-benzylindol-3-ylmethylene)quinuclidin-3-ols (1a-1k), (Z)-2-benzylindol-3-ylmethylene) quinuclidin-3-ones (2a-2h), (Z)-(+/-)-2-(1H/N-methyl-indol-3-ylmethylene) quinuclidin-3-ols (3a-3b), and substituted (Z)-(+/-)-2-(N-benzenesulfonylindol-3-yl-methylene) quinuclidin-3-ols and their derivatives (4a-4d) that incorporate a variety of substituents in both the indole and N-benzyl moieties was evaluated using Human Umbilical Vein Endothelial Cells (HUVECs) subjected to in vitro cell migration scratch assays, tubule formation in Matrigel, cell viability and proliferation assays. In total, 25 different analogs were evaluated. Based on in vitro cell migration scratch assays, eight analogs were identified as potent angiogenesis inhibitors at 10 mu M, a concentration that was determined to be nontoxic by colony formation assay. In addition, this approach identified a potent antiangiogenic ENOX1 inhibitor, analog 4b. (C) 2010 Elsevier Ltd. All rights reserved.
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Reference:
Quinuclidine – Wikipedia,
,Quinuclidine | C7H13N | ChemSpider