title: Synthesis and in Vitro Screening of New Series of 2,6-Dipeptidyl-anthraquinones: Influence of Side Chain Length on HIV-1 Nucleocapsid Inhibitors.
abstract: 2,6-Dipeptidyl-anthraquinones are a promising class of nucleic acid-binding compounds that act as NC inhibitors in vitro. We designed, synthesized, and tested new series of 2,6-disubstituted-anthraquinones, which are able to bind viral nucleic acid substrates of NC. We demonstrate here that these novel derivatives interact preferentially with noncanonical structures of TAR and cTAR, stabilize their dynamics, and interfere with NC chaperone activity.
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Frecentese
authors.affiliation: Dipartimento di Scienze del Farmaco, Università di Padova , via Marzolo 5, 35131 Padova, Italy.
authors.forename: Alice
authors.initials: A
authors.lastname: Sosic
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Irene
authors.initials: I
authors.lastname: Saccone
authors.affiliation: Dipartimento di Scienze del Farmaco, Università di Padova , via Marzolo 5, 35131 Padova, Italy.
authors.forename: Elia
authors.initials: E
authors.lastname: Gamba
authors.affiliation: Dipartimento di Scienze del Farmaco, Università di Padova , via Marzolo 5, 35131 Padova, Italy.
authors.forename: Kristina
authors.initials: K
authors.lastname: Link
authors.affiliation: Dipartimento di Scienze del Farmaco, Università di Padova , via Marzolo 5, 35131 Padova, Italy.
authors.forename: Angelica
authors.initials: A
authors.lastname: Miola
authors.affiliation: Dipartimento di Scienze del Farmaco, Università di Padova , via Marzolo 5, 35131 Padova, Italy.
authors.forename: Marta
authors.initials: M
authors.lastname: Cappellini
authors.affiliation: Dipartimento di Scienze del Farmaco, Università di Padova , via Marzolo 5, 35131 Padova, Italy.
authors.forename: Massimiliano Gianni
authors.initials: MG
authors.lastname: Cattelan
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Beatrice
authors.initials: B
authors.lastname: Severino
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Ferdinando
authors.initials: F
authors.lastname: Fiorino
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Elisa
authors.initials: E
authors.lastname: Magli
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Angela
authors.initials: A
authors.lastname: Corvino
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Elisa
authors.initials: E
authors.lastname: Perissutti
authors.affiliation: The RNA Institute and Department of Chemistry, State University of New York , 1400 Washington Avenue, Albany, New York 12222, United States.
authors.forename: Dan
authors.initials: D
authors.lastname: Fabris
authors.affiliation: Dipartimento di Scienze del Farmaco, Università di Padova , via Marzolo 5, 35131 Padova, Italy.
authors.forename: Barbara
authors.initials: B
authors.lastname: Gatto
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Caliendo
authors.affiliation: Dipartimento di Farmacia, Università di Napoli "Federico II" Via D. Montesano 49, 80131 Napoli, Italy.
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Santagada
mesh_terms: D000409:Alanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000880:Anthraquinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015497:HIV-1 / Q000737:chemistry / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D019251:Nucleocapsid / Q000037:antagonists & inhibitors* / Q000378:metabolism; D020218:Response Elements / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000880:Anthraquinones; D019380:Anti-HIV Agents; D000409:Alanine; D005998:Glycine