title: Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases.
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.
authors.affiliation: Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, P.le A. Moro 5, 00185 Roma, Italy. antonello.mai@uniroma1.it
authors.forename: Antonello
authors.initials: A
authors.lastname: Mai
authors.forename: Dante
authors.initials: D
authors.lastname: Rotili
authors.forename: Domenico
authors.initials: D
authors.lastname: Tarantino
authors.forename: Angela
authors.initials: A
authors.lastname: Nebbioso
authors.forename: Sabrina
authors.initials: S
authors.lastname: Castellano
authors.forename: Gianluca
authors.initials: G
authors.lastname: Sbardella
authors.forename: Marc
authors.initials: M
authors.lastname: Tini
authors.forename: Lucia
authors.initials: L
authors.lastname: Altucci
mesh_terms: D020650:Combinatorial Chemistry Techniques; D051548:Histone Acetyltransferases / Q000037:antagonists & inhibitors*; D006801:Humans; D006912:Hydroxyquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D050880:p300-CBP Transcription Factors / Q000037:antagonists & inhibitors*
chemical_list: D006912:Hydroxyquinolines; D051548:Histone Acetyltransferases; D050880:p300-CBP Transcription Factors