New chloro, fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action

被引：16
|
作者：
Ferro, Stefania [1 ]
De Luca, Laura [1 ]
Barreca, Maria Letizia [2 ]
De Grazia, Sara [1 ]
Christ, Frauke [3 ,4 ]
Debyser, Zeger [3 ,4 ]
Chimirri, Alba [1 ]
机构：
[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy
[2] Univ Perugia, Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy
[3] Katholieke Univ Leuven, B-3000 Louvain, Flanders, Belgium
[4] IRC KULAK, B-3000 Louvain, Flanders, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 15期
关键词：
HIV-1; integrase; Induced-fit docking; Integrase strand-transfer inhibitors; Microwave-assisted organic synthesis; REVERSE-TRANSCRIPTASE INHIBITORS; ANTI-HIV ACTIVITY; BINDING MODE; TN5; TRANSPOSASE; RALTEGRAVIR; UPDATE; POTENT; SITE; MECHANISM; DISCOVERY;
D O I：
10.1016/j.bmc.2010.06.063
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The life cycle of HIV-1 requires extensive assistance from the integrase (IN) enzyme which therefore constitutes an attractive therapeutic target for the development of anti-AIDS agents. We herein report the synthesis and biological evaluation of new HIV integrase strand-transfer inhibitors (INSTIs) which proved to be also potent anti-HIV agents. The binding mode of the most representative molecules were also studied by induced-fit docking (IFD). The obtained IFD results were consistent with the mechanism of action proposed for this class of IN inhibitors, that is metal chelating/binding agents. Crown Copyright (C) 2010 Published by Elsevier Ltd. All rights reserved.
引用
收藏
页码：5510 / 5518
页数：9
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