Novel Fluorinated Prodrugs for Activation by Carboxypeptidase G2 Showing Good in Vivo Antitumor Activity in Gene-Directed Enzyme Prodrug Therapy

Sixteen novel polyfluorinated benzoic acid mustards have been synthesized for use in gene-directed enzyme prodrug therapy (GDEPT). Eight of these were benzoic acid l-glutamate mustards for evaluation as prodrugs and the other eight were the active drugs formed by the action of the bacterial enzyme c...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-08, Vol.48 (16), p.5321-5328
Hauptverfasser:	Davies, Lawrence C, Friedlos, Frank, Hedley, Douglas, Martin, Jan, Ogilvie, Lesley M, Scanlon, Ian J, Springer, Caroline J
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic agents Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Biological and medical sciences Breast Neoplasms Cell Line, Tumor Drug Screening Assays, Antitumor Female Fluorine gamma-Glutamyl Hydrolase - genetics gamma-Glutamyl Hydrolase - metabolism General aspects Humans Medical sciences Mice Mice, Nude Mustard Compounds - chemical synthesis Mustard Compounds - chemistry Mustard Compounds - metabolism Mustard Compounds - pharmacology Neoplasm Transplantation Pharmacology. Drug treatments Prodrugs - chemical synthesis Prodrugs - chemistry Prodrugs - metabolism Prodrugs - pharmacology Structure-Activity Relationship Transplantation, Heterologous
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