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α-亚甲基内酯类肿瘤抑制剂与模型生物亲核试剂的反应。

Reactions of alpha methylene lactone tumor inhibitors with model biological nucelophiles.

作者信息

Kupchan S M, Fessler D C, Eakin M A, Giacobbe T J

出版信息

Science. 1970 Apr 17;168(3929):376-8. doi: 10.1126/science.168.3929.376.

DOI:10.1126/science.168.3929.376
PMID:5435896
Abstract

Thiols are the most reactive nucleophilic reagents among the biological models investigated. They undergo "Michael-type" addition to the polyfunctional sesquiterpene lactones. The rapid rates of reaction with L-cysteine were measured and the reaction products were characterized. Each addition of thiol successively decreased the cytotoxicity of the adducts formed.

摘要

硫醇是所研究的生物模型中反应活性最高的亲核试剂。它们会对多功能倍半萜内酯进行“迈克尔型”加成反应。测定了与L-半胱氨酸的快速反应速率，并对反应产物进行了表征。每次添加硫醇都会依次降低所形成加合物的细胞毒性。

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