41859-64-7Relevant academic research and scientific papers
Inhibition of ATP-sensitive K+-channels by a sulfonylurea analogue with a phosphate group
Hastedt, Katja,Panten, Uwe
, p. 599 - 602 (2003)
Hypoglycaemic sulfonylureas initiate insulin secretion by direct inhibition of ATP-sensitive K+-channels in the pancreatic β-cells. These channels are composed of two proteins, a pore-forming subunit (KIR6.2 in the case of β-cells) a
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.
Receptor Binding Sites of Hypoglycemic Sulfonylureas and Related benzoic Acids
Brown, George R.,Foubister, Alan J.
, p. 79 - 81 (2007/10/02)
The blood glucose level lowering activity of benzoic acid, such as p-benzoic acid (HB699, 2), is discussed in terms of binding at putative insulin-releasing receptor sites of pancreatic β cells.The hypoglycemic potencies fuond for synthetic analogues of 2 indicate that high hypoglycemic activity is only found when a carboxyl group or a group that is readily oxidized to carboxyl in vivo, such as methyl, is attached to the aromatic ring of the phenethyl group.It is proposed that this carboxyl group is able to bind at the same receptor site as the SO2NHCONH group of the sulfonylurea drugs, such as tolbutamide (3).The role of the benzamide group in 2 was attributed to protein binding.
