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1
Synthesis and anticancer activity evaluation of 3,4-mono- and bicyclosubstituted -(het)aryl trifluoromethyl succinimides.3,4-单取代和双环取代的-(杂)芳基三氟甲基琥珀酰亚胺的合成与抗癌活性评估
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2
Fluorine in pharmaceutical industry: fluorine-containing drugs introduced to the market in the last decade (2001-2011).制药行业中的氟：过去十年（2001 - 2011年）推向市场的含氟药物
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Synthesis, evaluation of anticancer activity and COMPARE analysis of N-bis(trifluoromethyl)alkyl-N'-substituted ureas with pharmacophoric moieties.含药效团的 N-双（三氟甲基）烷基-N’-取代脲的合成、抗癌活性评价及 COMPARE 分析。
Eur J Med Chem. 2012 Jul;53:364-73. doi: 10.1016/j.ejmech.2012.03.026. Epub 2012 Mar 23.
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Synthesis and anticancer activity of N-bis(trifluoromethyl)alkyl-N'-thiazolyl and N-bis(trifluoromethyl)alkyl-N'-benzothiazolyl ureas.N-双（三氟甲基）烷基-N'-噻唑基和 N-双（三氟甲基）烷基-N'-苯并噻唑基脲的合成及抗癌活性。
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3,3,3-三氟乙基异氰酸酯、氨基甲酸酯和脲的合成。-（3,3,3-三氟乙基）-' -取代脲的抗癌活性评估。

Synthesis of 3,3,3-trifluoroethyl isocyanate, carbamate and ureas. Anticancer activity evaluation of -(3,3,3-trifluoroethyl)-'-substituted ureas.

作者信息

Luzina Elena L, Popov Anatoliy V

机构信息

Institute of Physiologically Active Compounds, Severnyi pr. 1, Chernogolovka, Moscow region, 142432, Russia.

University of Pennsylvania, Perelman School of Medicine, Department of Radiology, 3620 Hamilton Walk, Philadelphia, PA 19104, USA.

出版信息

J Fluor Chem. 2015 Aug;176:82-88. doi: 10.1016/j.jfluchem.2015.06.005.

DOI:10.1016/j.jfluchem.2015.06.005
PMID:26213416
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4511494/
Abstract

A new method is described for producing 3,3,3-trifluoroethyl isocyanate from perfluoroisobutene (PFIB). Isocyanate was used for synthesis of carbamates and ureas. A series of trifluoroethyl-substituted ureas has been tested in the National Cancer Institute (NCI, Bethesda, USA) by the NCI-60 DTP Human Tumor Cell Line Screening Program at a single high dose (10 M). The moderate anticancer activity was shown against some types of cancer on the individual human cell lines for leukemia, non-small cell lung cancer and renal cancer.

摘要

描述了一种由全氟异丁烯（PFIB）制备3,3,3-三氟乙基异氰酸酯的新方法。异氰酸酯用于合成氨基甲酸酯和脲。美国国立癌症研究所（NCI，贝塞斯达）的NCI-60 DTP人类肿瘤细胞系筛选项目以单一高剂量（10 μM）对一系列三氟乙基取代的脲进行了测试。在个体人类细胞系上，对白血病、非小细胞肺癌和肾癌等某些类型的癌症显示出中等抗癌活性。