Original Articles

Antitumor action of phenylalanine derivatives of mechlorethamine

Jin-xu Zhou, Hui-zhen Liang, Bin Xu


The antitumor action and toxicity of 6 phenylalanine derivatives of mechlorethamine were compared in mice and rats. Ocaphane, o-[bis-(2-chloroethyl)-amino-methyl]-phenylalanine dihydrochloride (AT-581) was more potent than AT-290, AT-582, and mechlorethamine. Ocaphane showed a broader antitumor spectrum and less toxicity than the other compounds. The anti-tumor actions and toxicities of o-(AT-786) and m-(AT-916) tyrosine isomers of mechlorethamine were similar to ocaphane in mice. The toxicities of AT-786 and AT-916 in rats were higher, and thus their therapeutic indices in rats bearing Jensen sarcoma were less than that of ocaphane.
Nitrocaphane (AT-1258) was synthesized by introduction of a nitro group to position 5 of the benzene ring of ocaphane. Nitrocaphane was less toxic and more effective than ocaphane. The therapeutic index (LD50/ID50) of nitrocaphane in mice bearing Ehrlich carcinoma (solid form)=7, and its margin of safety (LD10/LD90)=2. About 62-86% of the rats bearing Jensen sarcoma could be cured by nitrocaphane alone.

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