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5-Substituted pyrimidine acyclic nucleoside analogues 1-cyanomethyl- and 1-(4-cyanobutyl)-5-substituted uracils as candidate antitumor agents

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Abstract

A number of 5-substituted pyrimidine acyclic nucleosides were synthesized and tested for in vitro cytotoxicity against four cell lines (J-82 cell, P-388 cell, FM-3A cell and U-938 cell lines). Synthesis of 1-cyanomethyl-5-substituted pyrimidines (1a-e) and 1-(4-cyanobutyl)-5-substituted pyrimidines (2a-e) was acomplished from the series of alkylation reactions of 5-substituted uracils with the corresponding chloroacetonitrile and 5-chlorovaleronitile in DMSO under 50°C temperature. These 5-substituted pyrimidine acylic nucleosides (1a-e and2a-e) exhibited moderate to significant activity against four cell lines.

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Kim, J.C., Dong, ES., Park, J.I. et al. 5-Substituted pyrimidine acyclic nucleoside analogues 1-cyanomethyl- and 1-(4-cyanobutyl)-5-substituted uracils as candidate antitumor agents. Arch. Pharm. Res. 17, 480–482 (1994). https://doi.org/10.1007/BF02979130

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