Effect of N-trifluoroacetyl derivatives of amino acids and amino acid analogs on microbial antitumor screen

Article abstract of DOI:10.1002/jps.2600680428

Eighteen trifluoroacetyl derivatives of amino acids and of amino acid analogs were prepared and tested for growth-inhibitory activity. Of the compounds tested, the trifluoroacetyl derivatives of o-, m-, and p-fluorophenylalanine and β-3-thienylalanine showed modest activity; trifluoroacetyl derivatives of phenylalanine and of β-2-thienylalanine showed marginal activity. The activity exhibited by the active trifluoroacetyl compounds was equal to that noted for most active chloroacetyl derivatives reported previously, as judged by comparison of their activity with that of chloroacetyl-m-fluorophenylalanine. No reversal of inhibition was noted when a representative of these inhibitors was challenged with a corresponding natural metabolite, both as free amino acid and as a noninhibitory acylated compound.