66217-29-6Relevant articles and documents
Structure-Activity Relationship Studies and Molecular Modeling of Naphthalene-Based Sphingosine Kinase 2 Inhibitors
Congdon, Molly D.,Kharel, Yugesh,Brown, Anne M.,Lewis, Stephanie N.,Bevan, David R.,Lynch, Kevin R.,Santos, Webster L.
, p. 229 - 234 (2016)
The two isoforms of sphingosine kinase (SphK1 and SphK2) are the only enzymes that phosphorylate sphingosine to sphingosine-1-phosphate (S1P), which is a pleiotropic lipid mediator involved in a broad range of cellular processes including migration, proliferation, and inflammation. SphKs are targets for various diseases such as cancer, fibrosis, and Alzheimer's and sickle cell disease. Herein, we disclose the structure-activity profile of naphthalene-containing SphK inhibitors and molecular modeling studies that reveal a key molecular switch that controls SphK selectivity.
Radical-induced ring-opening and reconstruction of cyclobutanone oxime esters
Wang, Panpan,Zhao, Binlin,Yuan, Yu,Shi, Zhuangzhi
, p. 1971 - 1974 (2019/05/02)
The first example of intramolecular ring-opening and reconstruction of cyclobutanone oxime esters via selective C-C bond cleavage leading to the synthesis of 3,4-dihydronaphthalene-2-carbonitriles in the presence of a cheap copper catalyst has been reported. The protocol is distinguished by mild and safe reaction conditions that exclude ligands, oxidants, bases, toxic cyanide salts and tolerates a wide scope of cyclobutanones without compromising their efficiency and scalability. The alternative visible-light-driven photoredox process for this coupling reaction was also uncovered.
SPHINGOSINE KINASE INHIBITOR AMIDOXIME PRODRUGS
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Page/Page column 233; 239, (2017/11/03)
Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides prodrugs of compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both, according to formula (I) as described herein. Formula I compounds are useful in the treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. The invention also provides pharmaceutical compositions of Formula I compounds.
SPHINGOSINE KINASE INHIBITORS
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Page/Page column 215; 221, (2016/04/26)
Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both. Certain compounds are selective for sphingosine kinase type 2 relative to sphingosine kinase type 1. Compounds of the invention can be used in treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. Diseases that can be treated by administration of an effective dose of a compound of the invention include a neoplastic disease that involves excess vascular growth; macular degeneration or diabetic retinopathy; an allergic disease such as asthma, an inflammatory disease of the eye such as uveitis, scleritis, or vitritis; an inflammatory disease of the kidney; a fibrotic disease; atherosclerosis; or pulmonary arterial hypertension. A compound of the invention can be used to improve the integrity of a vascular barrier in a disease where the vascular barrier is disrupted, such as cancer or Alzheimer's disease.
Multichromophoric cyclodextrins. 4. Light conversion by antenna effect
Jullien, Ludovic,Canceill, Josette,Valeur, Bernard,Bardez, Elisabeth,Lefèvre, Jean-Pierre,Lehn, Jean-Marie,Marchi-Artzner, Valérie,Pansu, Robert
, p. 5432 - 5442 (2007/10/03)
A water soluble β-cyclodextrin (CD-NA) bearing seven naphthoyl chromophores forms very stable 1:1 complexes with a merocyanine laser dye DCM-OH (4-(dicyanomethylene)-2-methyl-6-(p-(bis(hydroxyethyl)amino)-styryl)-4 H-pyran). The antenna effect, i.e. energ
