Structure/activity studies with thiazolidinyl- and perhydrothiazinylphosphamide ester.
Structure/activity studies were carried out with thiazolidinyl- and perhydrothiazinylphosphamide ester, which differ in the structure of the phosphamide moiety and in the rate of spontaneous hydrolysis to activated oxazaphosphorines. Antitumour activity in mice with advanced P388 tumours growing subcutaneously was increased 30- to 40-fold when one 2-chloroethyl group in l-aldophosphamide-perhydrothiazine was substituted by a mesylethyl group.
Zentrum der Biologischen Chemie der Johann Wolfgang Goethe-Universität, Frankfurt am Main, Germany.
G
G
Voelcker
H J
HJ
Hohorst
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005260:Female; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D009368:Neoplasm Transplantation; D010752:Phosphoramide Mustards / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology*
D000970:Antineoplastic Agents; D010752:Phosphoramide Mustards; D013844:Thiazoles