Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374450 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
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 α-tubulin. When tested in U937 cells, some compounds displayed pro-apoptotic or cytodifferentiating properties.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Antonello Mai, Dante Rotili, Domenico Tarantino, Angela Nebbioso, Sabrina Castellano, Gianluca Sbardella, Marc Tini, Lucia Altucci,