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

被引：13

作者：

Frecentese, Francesco ^{[1
]}

Sosic, Alice ^{[2
]}

Saccone, Irene ^{[1
]}

Gamba, Elia ^{[2
]}

Link, Kristina ^{[2
]}

Miola, Angelica ^{[2
]}

Cappellin, Marta ^{[2
]}

Cattelan, Massimiliano Gianni ^{[2
]}

Severino, Beatrice ^{[1
]}

Fiorino, Ferdinando ^{[1
]}

Magli, Elisa ^{[1
]}

Corvino, Angela ^{[1
]}

Perissutti, Elisa ^{[1
]}

Fabris, Dan ^{[3
,4
]}

Gatto, Barbara ^{[2
]}

Caliendo, Giuseppe ^{[1
]}

Santagada, Vincenzo ^{[1
]}

机构：

[1] Univ Naples Federico II, Dipartimento Farm, Via D Montesano 49, I-80131 Naples, Italy

[2] Univ Padua, Dipartimento Sci Farm, Via Marzolo 5, I-35131 Padua, Italy

[3] SUNY Albany, RNA Inst, 1400 Washington Ave, Albany, NY 12222 USA

[4] SUNY Albany, Dept Chem, 1400 Washington Ave, Albany, NY 12222 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 59卷 / 05期

关键词：

HELIX-THREADING PEPTIDES; HUMAN-IMMUNODEFICIENCY-VIRUS; REVERSE TRANSCRIPTION; STRAND TRANSFER; RNA; PROTEIN; BINDING; DISCOVERY; COMPLEX;

D O I：

10.1021/acs.jmedchem.5b01494

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1914 / 1924

页数：11

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