[N-phosphorylated amino acids as potential cytostatics].
Phosphoramidic dichlorides 3 are synthesized by nucleophilic attack of methyl 2-(1-ethylenimino)-alkanoates 1 on POCl3 or by the reaction of amino acid methyl ester hydrochlorides 2 with POCl3. Subsequent treatment of 3 with ethylenimine affords the TEPA-analogs 4, and with 3-(1-ethylenimino)-1-propanol (6) the IFOSFAMID analogous 1,3,2-oxaza-phosphorines 5, the cytostatic activity of which was tested in the P388-leukemia of the CD2F1-mouse.
Schwieger
J F
JF
Institut für Pharmazeutische Chemie, Westfälischen Wilhelms-Universität, Münster.
Unterhalt
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B
D000596:Amino Acids / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D010766:Phosphorylation
D000596:Amino Acids; D000970:Antineoplastic Agents
N-Phosphorylierte Aminosäuren als potentielle Zytostatika.