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Synthesis and cytotoxic activity of heterocyclization products of 1,1-dicyano-2-hetaryl-2-trifluoromethylethylenes
Authors:Yu E Pavlova  A F Shidlovskii  D B Gusev  A S Peregudov  Yu N Bulychev  N D Chkanikov
Institution:1.A. N. Nesmeyanov Institute of Organoelement Compounds,Russian Academy of Sciences,Moscow,Russian Federation;2.Research institute of Experimental Diagnostics and Tumor Therapy N. N. Blokhin Russian Cancer Research Center,Russian Academy of Medical Sciences,Moscow,Russian Federation
Abstract:Methods for the synthesis of novel fluorinated compounds by reaction of 1,1-dicyano-2-hetaryl-2-trifluoromethylethylenes with a variety of nitrogen heterocycles have been developed. Cyctotoxicity of the obtained organofluorine heterocycles were studied in vitro at the U.S. National Cancer Institute (NCI) in the framework of the International Program for Development of Effective Antitumor Drugs. Cytotoxic activity in the series of fluorinated pyrazolo1,5-a]pyrimidines has been observed for the first time, this strongly depending on the nature and position of the substituents.
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