Ethacrynic acid analogues lacking the alpha,beta-unsaturated carbonyl unit--potential anti-metastatic drugs.

Autor: Janser RF; Laboratory of Organic Synthesis, Catalysis and Biochemistry (LOSCB), Department of Chemistry, New Mexico Institute of Mining and Technology, Socorro, NM 87801, USA., Meka RK, Bryant ZE, Adogla EA, Vogel EK, Wharton JL, Tilley CM, Kaminski CN, Ferrey SL, Van Slambrouck S, Steelant WF, Janser I
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Mar 15; Vol. 20 (6), pp. 1848-50. Date of Electronic Publication: 2010 Feb 02.
DOI: 10.1016/j.bmcl.2010.01.144
Abstrakt: A series of ethacrynic acid analogues, lacking the alpha,beta-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.
(Copyright 2010 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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