4.7 Article

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

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 59, Issue 5, Pages 1914-1924

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01494

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Funding

  1. MIUR [PRIN: 2010W2KM5L_006]
  2. MAECI, Ministero Affari Esteri e Cooperazione Internazionale [PGR00171]

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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.

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