2887-55-0Relevant articles and documents
HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
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Page/Page column 102, (2015/01/16)
The present invention provides, in part, compounds of Formula (I) and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1 -mediated (or D1 -associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.
Inhibitory effects of ethacrynic acid analogues lacking the α,β-unsaturated carbonyl unit and para-acylated phenols on human cancer cells
Bryant, Zack E.,Janser, Romy F.J.,Jabarkhail, Medina,Candelaria-Lyons, Melissa S.,Romero, Brittni B.,Slambrouck, Severine Van,Steelant, Wim F.A.,Janser, Ingo
scheme or table, p. 912 - 915 (2011/03/21)
A series of ethacrynic acid analogues, lacking the α,β- unsaturated carbonyl unit, was synthesized and subsequently evaluated for their ability to inhibit the migration of human breast cancer cells, Hs578Ts(i)8 as well as of human prostate cancer cells, C4-2B. These cell lines provide a good model system to study migration and invasion, since they represent metastatic cancer. Our studies show that ethacrynic acid analogues with methyl substituents at the aromatic ring demonstrate no inhibitory effect on the migration of both cancer cell lines, whereas a precursor in the synthesis of these ethacrynic acid analogues (II-1, a para-acylated m-cresol) is an excellent inhibitor of the migration of both cancer cell lines.
Ethacrynic acid analogues lacking the α,β-unsaturated carbonyl unit-Potential anti-metastatic drugs
Janser, Romy F.J.,Meka, Ranjith K.,Bryant, Zack E.,Adogla, Enoch A.,Vogel, Elizabeth K.,Wharton, Jaimie L.,Tilley, Cynthia M.,Kaminski, Catherine N.,Ferrey, Seth L.,Van slambrouck, Severine,Steelant, Wim F.A.,Janser, Ingo
experimental part, p. 1848 - 1850 (2010/07/06)
A series of ethacrynic acid analogues, lacking the α,β-unsaturated carbonyl unit, was synthesized and subsequently evaluated for their ability to inhibit the migration of human breast cancer cells, MCF-7/AZ. Several of the analogues were already active in the low micromolar range, whereas ethacrynic acid itself shows no potential to inhibit the migration of these cancer cells. Preliminary studies show that the presence of one or more methoxy groups at the phenyl ring of ethacrynic acid is important in order for the ethacrynic acid analogues to demonstrate an inhibitory effect on the migration.
