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.
Mai, A., Rotili, D., Tarantino, D., Angela, N., Sabrina, C., Gianluca, S., et al. (2009). Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 19(4), 1132-1135 [10.1016/j.bmcl.2008.12.097].
Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases
ROTILI, Dante;
2009-01-01
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.