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[Alkylating derivatives of 2-amino-2-desoxy-1,3,4,6-tetraacetyl-D-glucopyranose (synthesis and experimental study)].

The writers report the results of synthesis and experimental studies of 2-amino-2-desoxy-1, 3, 4, 6-tetraacetyl-D-glucopyranose derivatives acylated by n-di-/2-chloroethyl/aminophenyl acetic acid (chlorophenacyl), n-di-/2-chloroethyl/aminophenyl-N-acetyl-DL-alanine (acetylsarcolysin) and n-di-/2-chloroethyl/aminophenyl-N-acetyl-DL-alanyl-DL-valine (acetylsarcolysin valine). Studies on the antitumor activity were carried out on mice with 8 different transplantable tumors. The addition of glucosamine to alkylating substances containing biologically active components was found to change their properties. The new type derivatives are watersoluble, show less molar toxicity and mainly high activity on plasmocytoma MOPC-406 (from 97% of the survival rate to 50% of cure).

Alkylating Agents↗