Of 49 compounds known to have antitumor properties, 6 were found to have significant activity against Trypanosoma rhodesiense infections in mice. Activity against the African trypanosomes has not been reported previously for any of these six compounds. In order of decreasing activity these compounds were: (i) imidazole-4-carboxamide, 5-(3,3-dimethyl-1,1-triazene), (ii) inosine diglycolaldehyde, (iii) cis-diamminedichloro-platinum, (iv) streptozotocin, (v) coralyne sulfate, and (vi) 5-fluoro-2'-deoxyuridine. The percentage of "hits" (12.2%) from these known antitumor agents was approximately twice as great as when other means are employed for the selection of compounds for this test system.
Antitrypanosomal activity for benzyltriphenylphosphonium salts is reported for the first time. Testing was conducted using Trypanosoma rhodesiense infected mice. Of 70 phosphorus-containing compounds tested, 21 were active. Sixteen of these active chemical species were benzyltriphenylphosphonium salts. Four were nonbenzyl triphenyl compounds. The remaining active drug was a benzyldiphenylphosphonium salt.
Of 303 compounds (66 active against cancer and 237 inactive against cancer) obtained from the Drug Synthesis and Chemistry Branch, Developmental Therapeutics Program, Division of Cancer Treatment, National Cancer Institute, Bethesda, Maryland, 25 were found to be active against Trypanosoma rhodesiense infections of ICR/Ha Swiss mice. Fifteen of these 25 compounds also had anticancer properties. The percentage of anticancer compounds found to have antitrypanosomiasis properties was 22.7. This percentage compares with 6% antitrypanosomiasis compounds among compounds selectecd by other methods.
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