Synthesis and anticancer activity evaluation of 3,4-mono- and bicyclosubstitutedN-(het)aryl trifluoromethyl succinimides.
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,band6a-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 (10-5M). 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).
Institute of Physiologically Active Compounds, Severnyi pr. 1, Chernogolovka, Moscow region, 142432, Russia.
Elena L
EL
Luzina
University of Pennsylvania, Perelman School of Medicine, Department of Radiology, 3620 Hamilton Walk, Philadelphia, PA 19104, USA.
Anatoliy V
AV
Popov
anticancer activity; cycloaddition; cyclocondensation; fluorinated heterocycles; synthesis; trifluoromethyl succinimides; trifluoromethylmaleic anhydride