Exploring the potential of the β-thiolactones in bioorganic chemistry

被引:16
作者
Aubry, Sylvain [1 ]
Sasaki, Kaname [1 ]
Eloy, Laure [1 ]
Aubert, Genevieve [1 ]
Retailleau, Pascal [1 ]
Cresteil, Thierry [1 ]
Crich, David [1 ]
机构
[1] CNRS, Inst Chim Subst Nat, Ctr Rech Gif, F-91190 Gif Sur Yvette, France
关键词
CYSTEINE PROTEINASE-INHIBITORS; FREE-RADICAL CHEMISTRY; PROTEASOME INHIBITORS; SALINOSPORAMIDE-A; MOLECULAR-STRUCTURE; COUPLING REACTIONS; CANCER-THERAPY; ACTIVE-SITE; CATHEPSIN-B; LACTONES;
D O I
10.1039/c1ob05967j
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of novel peptide-based beta-thiolactones were synthesized and assayed for cytotoxicity against several human cancer cell lines, where they showed greater activity than the corresponding beta-lactones and beta-lactams. Several of the beta-thiolactones prepared showed strong inhibitory activity in vitro against human cathepsins B and L.
引用
收藏
页码:7134 / 7143
页数:10
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