In order to gather further knowledge about the structural requirements on histone deacetylase inhibitors (HDACi), starting from the schematic model of the common pharmacophore that characterizes this class of molecules (surface recognition CAP group-connection unit-linker region-Zinc Binding Group), we designed and synthesized a series of hydroxamic acids containing a bis-(indolyl) methane moiety. HDAC inhibition pro. le and antiproliferative activity were evaluated. (C) 2009 Elsevier Ltd. All rights reserved.
Giannini G, Marzi M, Di Marzo M, Battistuzzi G, Pezzi R, Brunetti T, et al. (2009). Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 19(10), 2840-2843 [10.1016/j.bmcl.2009.03.101].
Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors
Cabri W;
2009
Abstract
In order to gather further knowledge about the structural requirements on histone deacetylase inhibitors (HDACi), starting from the schematic model of the common pharmacophore that characterizes this class of molecules (surface recognition CAP group-connection unit-linker region-Zinc Binding Group), we designed and synthesized a series of hydroxamic acids containing a bis-(indolyl) methane moiety. HDAC inhibition pro. le and antiproliferative activity were evaluated. (C) 2009 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
