| Abstrakt: |
Twenty-seven N-benzoyl derivatives of amino acids and amino acid analogs were prepared and tested for growth-inhibitory activity in a microbial antitumor screen. Of these, 19 showed some inhibitory capacity, from a modest 13% to a potent 96% at 1 mg/ml. The activities of the "modest" inhibitors were comparable to those of most inhibitory chloracetyl and trifluoroacetyl derivatives reported earlier. The intermediate inhibitors were as active as N-chloroacetyl-beta-hydroxy-D-norleucine isomer B, the most active acyl derivative noted previously. The most active compounds in this study were N-benzoyl-p-chloro-DL-phenylalanine and N-benzoyl-m-fluoro-DL-phenylalanine, which inhibited the test organism almost completely under the assay conditions. |
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