期刊
JOURNAL OF FLUORINE CHEMISTRY
卷 168, 期 -, 页码 121-127出版社
ELSEVIER SCIENCE SA
DOI: 10.1016/j.jfluchem.2014.09.019
关键词
Trifluoromethylmaleic anhydride; Trifluoromethyl succinimides; Fluorinated heterocycles; Cycloaddition; Cyclocondensation; Anticancer activity; Synthesis
资金
- National Center for Advancing Translational Sciences of the National Institutes of Health [UL1TR000003]
Novel trifluoromethylated mono- and bicyclic succinimides derived from trifluoromethylmaleic anhydride were synthesized using cyclopentadiene or 2,3-dimethylbutadiene and (het)arylamines. The biological activity of these compounds was evaluated using prediction methods and experimental studies. This series of new trifluoromethyl succinimides (3a,b and 6a-c) were tested by the National Cancer Institute (NCI, Bethesda, USA) by Program NCI-60 DTP Human Tumor Cell Line Screen at a single high dose (10(-5) M). Imides revealed activity on Leukemia cell lines (RPMI-8226 - myeloma cell line), Non-Small Cell Lung Cancer cell lines (A549/ATCC - lung carcinoma epithelial cells) and Renal cancer cell lines (A498 and SN12 C). (C) 2014 Elsevier B.V. All rights reserved.
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