Synthesis and in Vitro Screening of New Series of 2,6-Dipeptidyl-anthraquinones: Influence of Side Chain Length on HIV-1 Nucleocapsid Inhibitors
| Autor: | 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 |
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| Přispěvatelé: | 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 |
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
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 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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