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卤代二芳基乙炔可抑制癌细胞中c-myc的表达。

Halogenated diarylacetylenes repress c-myc expression in cancer cells.

作者信息

Sviripa Vitaliy M, Zhang Wen, Kril Liliia M, Liu Alice X, Yuan Yaxia, Zhan Chang-Guo, Liu Chunming, Watt David S

机构信息

Department of Molecular and Cellular Biochemistry, College of Medicine, University of Kentucky, Lexington, KY 40536-0509, United States; Center for Pharmaceutical Research and Innovation, College of Pharmacy, University of Kentucky, Lexington, KY 40536-0596, United States.

Department of Molecular and Cellular Biochemistry, College of Medicine, University of Kentucky, Lexington, KY 40536-0509, United States; Lucille Parker Markey Cancer Center, University of Kentucky, Lexington, KY 40536-0093, United States.

出版信息

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3638-40. doi: 10.1016/j.bmcl.2014.04.113. Epub 2014 May 9.

DOI:10.1016/j.bmcl.2014.04.113
PMID:24930834
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4096707/
Abstract

Halogenated diarylacetylenes that possess fluorine or chlorine substituents in one aryl ring and N-methylamino or N,N-dimethylamino in the other aryl ring inhibit the proliferation of LS174T colon cancer cells through the repression of c-myc expression and induction of the cyclin-dependent kinase inhibitor-1 (i.e., p21(Wif1/Cip1)) and represent potentially useful antineoplastic agents.

摘要

在一个芳基环中具有氟或氯取代基且在另一个芳基环中具有N-甲基氨基或N，N-二甲基氨基的卤代二芳基乙炔通过抑制c-myc表达和诱导细胞周期蛋白依赖性激酶抑制剂-1（即p21（Wif1/Cip1））来抑制LS174T结肠癌细胞的增殖，是潜在有用的抗肿瘤药物。

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