64353-17-9Relevant articles and documents
Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity
Kabro, Anzhelika,Lachance, Hugo,Marcoux-Archambault, Iris,Perrier, Valerie,Dore, Vicky,Gros, Christina,Masson, Veronique,Gregoire, Jean-Marc,Ausseil, Frederic,Cheishvili, David,Laulan, Nathalie Bibens,St-Pierre, Yves,Szyf, Moshe,Arimondo, Paola B.,Gagnon, Alexandre
, p. 1562 - 1570 (2013/12/04)
DNA-methyltransferases (DNMTs) are a class of epigenetic enzymes that catalyze the transfer of a methyl moiety from the methyl donor S-adenosyl-l-methionine onto the C5 position of cytosine in DNA. This process is dysregulated in cancers and leads to the hypermethylation and silencing of tumor suppressor genes. The development of potent and selective inhibitors of DNMTs is of utmost importance for the discovery of new therapies for the treatment of cancer. We report herein the synthesis and DNMT inhibitory activity of 29 analogues derived from NSC 319745. The effect of selected compounds on the methylation level in the MDA-MB-231 human breast cancer cell line was evaluated using a luminometric methylation assay. Molecular docking studies have been conducted to propose a binding mode for this series.
Acylamino(alkyl)benzene derivatives and process for preparing them
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, (2008/06/13)
The invention relates to acylamino(alkyl)benzene derivatives of the general formula STR1 in which W represents a group which can be converted into a carboxyl group, or an aldehyde group or an oxymethyl group or their derivatives or also a low molecular weight alkyl group, preferably a methyl group, X represents an aromatic or hetero-aromatic ring system, Y represents a single chemical bond or a hydrocarbon bridge, and Z represents hydrogen or one or even several other substituents, To their preparation and to pharmaceutical compositions containing them. The compounds have blood sugar lowering activity and may be used in the therapy of diabetes mellitus.