Solution Phase Synthesis of a Combinatorial Library of Chalcones and Flavones as Potent Cathepsin V Inhibitors

被引：31

作者：

Alvim, Joel, Jr. ^{[1
]}

Severino, Richele P. ^{[1
,2
]}

Marques, Emerson F. ^{[1
]}

Martinelli, Ariane M. ^{[1
]}

Vieira, Paulo C. ^{[1
]}

Fernandes, Joao B. ^{[1
]}

da Silva, M. Fatima das G. F. ^{[1
]}

Correa, Arlene G. ^{[1
]}

机构：

[1] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP, Brazil

[2] Univ Fed Goias, Dept Quim, BR-75704020 Catalao, Go, Brazil

来源：

JOURNAL OF COMBINATORIAL CHEMISTRY | 2010年 / 12卷 / 05期

关键词：

ENVIRONMENTALLY BENIGN SYNTHESIS; PARALLEL SYNTHESIS; ANTIMALARIAL ACTIVITY; PRIVILEGED STRUCTURES; DERIVATIVES; ANTIBACTERIAL; BIOSYNTHESIS; EFFICIENT; ANALOGS; DESIGN;

D O I：

10.1021/cc100076k

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Cathepsin V is a papain-like cysteine protease. It is involved in the control of human T cells (responsible for cell immunity), and presents the largest elastolytic activity among the proteolytic enzymes. Therefore, cathepsin V is a potential molecular target for the treatment of atherosclerosis. In the present work, natural flavonoids were screened against cathepsin V, and two flavones were identified as potent inhibitors of cathepsin V. On the basis of this result, a combinatorial library of chalcones and flavones was prepared, in solution phase employing a scavenger reagent, and fully evaluated.

引用

页码：687 / 695

页数：9

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