Synthesis and anticancer activity evaluation of 3,4-mono- and bicyclosubstituted -(het)aryl trifluoromethyl succinimides.

J Fluor Chem

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

Published: December 2014

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 ( and ) 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 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 SN12C).

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4230577PMC
http://dx.doi.org/10.1016/j.jfluchem.2014.09.019DOI Listing

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