Bioreductively Activated Lysyl Oxidase Inhibitors against Hypoxic Tumours

被引:22
作者
Granchi, Carlotta [1 ]
Funaioli, Tiziana [2 ]
Erler, Janine T. [3 ]
Giaccia, Amato J. [3 ]
Macchia, Marco [1 ]
Minutolo, Filippo [1 ]
机构
[1] Univ Pisa, Dipartimento Sci Farmaceut, I-56126 Pisa, Italy
[2] Univ Pisa, Dipartimento Chim & Chim Ind, I-56126 Pisa, Italy
[3] Stanford Univ, Dept Radiat Oncol, Sch Med, Stanford, CA 94305 USA
关键词
antitumor agents; cancer; electrochemical potential; hypoxia; lysyl oxidase; prodrugs; BETA-AMINOPROPIONITRILE; METASTASIS; CYTOTOXICITY; MECHANISMS; CELLS;
D O I
10.1002/cmdc.200900247
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
(Figure Presented) The right keys for tumour locks: Nitroaromatic and heteroaromatic portions are suitably sensitive to hypoxic conditions when used as BAPN masking groups, and the resulting prodrugs (pro-BAPNs) showed good levels of in vitro hypoxia-selective inhibition of lysyl oxidase (LOX) activity and cancer cell invasion. © 2009 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:1590 / 1594
页数:5
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