Showdomycin analogs: synthesis and antitumor evaluation

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Abstract
The synthesis of N-.beta.-D-ribofuranosyl derivatives of maleimide, 3-methylmaleimide and 3-chloromaleimide was accomplished in 3 steps from ribosylamine. The synthetic ribosides can be considered N-nucleoside analogs to showdomycin, which is an antitumor antibiotic of the C-nucleoside type. Although the 3 analogs were cytotoxic to cultured L1210 [mouse leukemia] cells, no in vivo antitumor activity was found with the murine P388 leukemia test system. Drug transport studies were done in an attempt to trace the biological fate of the analogs.