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NSC 670224 的结构测定、类似物的合成及生物学评价。

Structural determination of NSC 670224, synthesis of analogues and biological evaluation.

机构信息

Department of Chemistry and Biochemistry, University of California, Santa Cruz (UCSC), Santa Cruz, CA 95064, USA.

出版信息

ChemMedChem. 2012 May;7(5):761-5. doi: 10.1002/cmdc.201200038. Epub 2012 Feb 29.

DOI:10.1002/cmdc.201200038
PMID:22378491
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3516922/
Abstract

Follow my lead! NSC 670224, previously shown to be toxic to Saccharomyces cerevisiae at low micromolar concentrations, potentially acts via a mechanism of action related to that of tamoxifen (NSC 180973), breast cancer drug. The structure of NSC 670224, previously thought to be a 2,4-dichloro arene, was established as the 3,4-dichloro arene, and a focused library of analogues were synthesized and biologically evaluated.

摘要

跟我来！NSC 670224 先前在低微摩尔浓度下对酿酒酵母显示出毒性，可能通过与他莫昔芬（NSC 180973）相关的作用机制发挥作用，他莫昔芬是一种乳腺癌药物。先前被认为是 2,4-二氯芳烃的 NSC 670224 的结构被确定为 3,4-二氯芳烃，并合成和生物评估了一个聚焦的类似物文库。