We identified a series of 4-hydroxyquinolines bearing a C1 to C15 alkyl chain at the C2 position and a carbethoxy/carboxy group at the C3 position of the quinoline nucleus (MC compounds), endowed with selective inhibitory activity against the p300/CBP HAT enzymes. Enzyme inhibition was investigated using in vitro HAT assays and by western blot analysis of cellular lysates to examine the acetylation levels of histone H3 and alpha-tubulin. When tested in U937 cells, some compounds displayed pro-apoptotic or cytodifferentiating properties. (C) 2009 Elsevier Ltd. All rights reserved.
Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases / Mai, Antonello; Rotili, Dante; Tarantino, Domenico; Angela, Nebbioso; Sabrina, Castellano; Gianluca, Sbardella; Marc, Tini; Lucia, Altucci. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 19:4(2009), pp. 1132-1135. [10.1016/j.bmcl.2008.12.097]
Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases
MAI, Antonello;ROTILI, Dante;TARANTINO, DOMENICO;
2009
Abstract
We identified a series of 4-hydroxyquinolines bearing a C1 to C15 alkyl chain at the C2 position and a carbethoxy/carboxy group at the C3 position of the quinoline nucleus (MC compounds), endowed with selective inhibitory activity against the p300/CBP HAT enzymes. Enzyme inhibition was investigated using in vitro HAT assays and by western blot analysis of cellular lysates to examine the acetylation levels of histone H3 and alpha-tubulin. When tested in U937 cells, some compounds displayed pro-apoptotic or cytodifferentiating properties. (C) 2009 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
