Preclinical evaluation of amino acid prodrugs of novel antitumor 2-(4-amino-3-methylphenyl)benzothiazoles.

  title={Preclinical evaluation of amino acid prodrugs of novel antitumor 2-(4-amino-3-methylphenyl)benzothiazoles.},
  author={Tracey D Bradshaw and Michael Charles Bibby and John A. Double and Iduna Fichtner and Patricia A. Cooper and Michael C. Alley and Susan Donohue and Sherman F. Stinson and Joseph E Tomaszewjski and Edward A. Sausville and Malcolm F. G. Stevens},
  journal={Molecular cancer therapeutics},
  volume={1 4},
Novel 2-(4-aminophenyl)benzothiazoles (e.g., compounds 1 and 2) possess highly selective, potent antitumor properties in vitro and in vivo. Elucidation of the mechanism of action of this structurally simple class of compounds has occurred in parallel with selection of a candidate clinical agent. Antitumor benzothiazoles induce and are biotransformed by cytochrome P 450 1A1 to putative active, as well as inactive metabolites. Metabolic inactivation of the molecule has been thwarted by isosteric… CONTINUE READING
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