A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors

被引：100

作者：

Chimenti, Franco ^{[1
]}

Fioravanti, Rossella ^{[1
]}

Bolasco, Adriana ^{[1
]}

Chimenti, Paola ^{[1
]}

Secci, Daniela ^{[1
]}

Rossi, Francesca ^{[1
]}

Yanez, Matilde ^{[2
,3
]}

Orallo, Francisco ^{[2
,3
]}

Ortuso, Francesco ^{[4
]}

Alcaro, Stefano ^{[4
]}

Cirilli, Roberto ^{[5
]}

Ferretti, Rosella ^{[5
]}

Sanna, M. Luisa ^{[5
]}

机构：

[1] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farmaco, I-00185 Rome, Italy

[2] Univ Santiago de Compostela, Dept Farmacol, E-15782 La Coruna, Spain

[3] Univ Santiago de Compostela, Fac Farm, Inst Farm Ind, E-15782 La Coruna, Spain

[4] Univ Catanzaro Magna Graecia, Dipartimento Sci Farmacobiol, I-88021 Roccelletta Di Borgia, CZ, Italy

[5] Ist Super Sanita, Dipartimento Farmaco, I-00161 Rome, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 03期

关键词：

Flavones; MAO inhibitors; Molecular modeling; Enantiomeric separation; CANCER; INFLAMMATION; POLYPHENOLS; QUERCETIN;

D O I：

10.1016/j.bmc.2009.12.029

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

A new series of synthetic flavones, thioflavones, and flavanones has been synthesized and evaluated as potential inhibitors of monoamine oxidase isoforms (MAO-A and -B). The most active series is the flavanone one with higher selective inhibitory activity against MAO-B. Some of these flavanones (mainly the most effective) have been separated and tested as single enantiomers. In order to investigate the MAOs recognition of the most active and selective compounds, a molecular modeling study has been performed using available Protein Data Bank (PDB) structures as receptor models for docking experiments. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1273 / 1279

页数：7

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