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作为选择性明胶酶抑制剂的手性2-(4-苯氧基苯基磺酰甲基)硫杂环丙烷的合成。

Synthesis of chiral 2-(4-phenoxyphenylsulfonylmethyl)thiiranes as selective gelatinase inhibitors.

作者信息

Lee Mijoon, Bernardo M Margarida, Meroueh Samy O, Brown Stephen, Fridman Rafael, Mobashery Shahriar

机构信息

Department of Chemistry and Biochemistry and the Walther Cancer Research Center, University of Notre Dame, Notre Dame, Indiana 46556, USA.

出版信息

Org Lett. 2005 Sep 29;7(20):4463-5. doi: 10.1021/ol0517269.

DOI:10.1021/ol0517269
PMID:16178559
Abstract

[reactions: see text] Compound 1, 2-(4-phenoxyphenylsulfonylmethyl)thiirane, is a selective inhibitor of gelatinases, which is showing high promise in studies of animal models for cancer metastasis and stroke. The (R)-1 and (S)-1 enantiomers of compound 1 were each synthesized in this study and were shown to be equally active in inhibition of gelatinases.

摘要

[反应:见正文] 化合物1,2-(4-苯氧基苯基磺酰甲基)硫杂环丙烷,是一种明胶酶的选择性抑制剂,在癌症转移和中风动物模型研究中显示出很高的前景。本研究中分别合成了化合物1的(R)-1和(S)-1对映体,并显示它们在抑制明胶酶方面具有同等活性。

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