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3. Synthesis and in Vitro Screening of New Series of 2,6-Dipeptidyl-anthraquinones: Influence of Side Chain Length on HIV-1 Nucleocapsid Inhibitors

Author

Frecentese, Francesco, primary, Sosic, Alice, additional, Saccone, Irene, additional, Gamba, Elia, additional, Link, Kristina, additional, Miola, Angelica, additional, Cappellini, Marta, additional, Cattelan, Massimiliano Gianni, additional, Severino, Beatrice, additional, Fiorino, Ferdinando, additional, Magli, Elisa, additional, Corvino, Angela, additional, Perissutti, Elisa, additional, Fabris, Dan, additional, Gatto, Barbara, additional, Caliendo, Giuseppe, additional, and Santagada, Vincenzo, additional more...

Published
2016
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4. Synthesis and in Vitro Screening of New Series of 2,6-Dipeptidyl-anthraquinones: Influence of Side Chain Length on HIV-1 Nucleocapsid Inhibitors

Author

Marta Cappellini, Elisa Magli, Barbara Gatto, Giuseppe Caliendo, Vincenzo Santagada, Elia Gamba, Angelica Miola, Kristina Link, Alice Sosic, Irene Saccone, Dan Fabris, Beatrice Severino, Angela Corvino, Massimiliano Gianni Cattelan, Francesco Frecentese, Ferdinando Fiorino, Elisa Perissutti, 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, and Santagada, Vincenzo more...

Subjects
0301 basic medicine, Anti-HIV Agents, Stereochemistry, Drug Evaluation, Preclinical, Glycine, Anthraquinones, Microbial Sensitivity Tests, Response Elements, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, Drug Discovery, Side chain, Structure–activity relationship, Binding site, Nucleocapsid, Alanine, Binding Sites, Dose-Response Relationship, Drug, Molecular Structure, Drug Discovery3003 Pharmaceutical Science, In vitro, 030104 developmental biology, chemistry, Molecular Medicine, HIV-1, Nucleic acid
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. more...

Published
2016