Nitrosourea derivatives

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Recombinant or stably-transformed bacterium encoding one or...

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564 33, A61K 3117, C07C12716

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active

044528140

ABSTRACT:
Nitrosourea derivatives are provided which possess a high level of inhibitory activity against leukemia and tumors and which are therefore useful for pharmaceutical purposes. The compounds have the structure represented by formulae (I), (II) and (III): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.4 may be the same or different and each represent a hydrogen atom or an alkyl, aryl, aralkyl, alkanoyl or a heterocyclic group; R.sup.3 represents the residual group on the .alpha.-carbon atom of an .alpha.-amino acid; n represents 2 or 3; X represents a halogen atom selected from chlorine, fluorine and bromine; and Ac represents an alkanoyl group.

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Zeller et al., "Chemotherapeutic Activity of 2-Chloroethylnitrosocarbamoyl Derivatives of Amino Acids in a Transplanted Rat Leukemia" (L5222) Drug Res. 32(I) 1982.
Tang et al., "Synthesis of Potentially Antineoplastic Derivatives of N-[N-(2-Cloroethyl)-N-Nitrosocarbamoyl]Amino Acids" Arch. Pharm., vol. 314, 1981.
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