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
Synthesis and in Vitro Screening of New Series of 2,6-Dipeptidyl-anthraquinones: Influence of Side Chain Length on HIV-1 Nucleocapsid Inhibitors / Frecentese, Francesco; Sosic, Alice; Saccone, Irene; Gamba, Elia; Link, Kristina; Miola, Angelica; Cappellini, Marta; Cattelan, Massimiliano Gianni; Severino, Beatrice; Fiorino, Ferdinando; Magli, Elisa; Corvino, Angela; Perissutti, Elisa; Fabris, Dan; Gatto, Barbara; Caliendo, Giuseppe; Santagada, Vincenzo. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 59:5(2016), pp. 1914-1924. [10.1021/acs.jmedchem.5b01494]
Synthesis and in Vitro Screening of New Series of 2,6-Dipeptidyl-anthraquinones: Influence of Side Chain Length on HIV-1 Nucleocapsid Inhibitors
FRECENTESE, FRANCESCO;SACCONE, IRENE;SEVERINO, BEATRICE;FIORINO, FERDINANDO;MAGLI, ELISA;CORVINO, ANGELA;PERISSUTTI, ELISA;CALIENDO, GIUSEPPE;SANTAGADA, VINCENZO
2016
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 activityFile | Dimensione | Formato | |
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