Synthesis of phosphoramide mustard analogues of daunomycin and carminomycin.
New phosphoramide mustards (6-8) have been prepared from the antibiotics 2 and 3, and from 5. The mixture of cyclophosphamides could be separated by preparative layer and column chromatography. The assignments of configuration to the isomeric phosphoramidates was based on the magnetic anisotropy of the P = O bond. The synthesized compounds 6a,b-8a,b (mixture of isomers) were tested for inhibitory activity on the [3H]-thymidine incorporation into the DNA of tumor cells, using ovarian carcinoma cell line.
Csorvási
A
A
Research Group for Antibiotics of the Hungarian Academy of Sciences, L. Kossuth University, Debrecen, Hungary.
Kövér
K E
KE
Menyhárt
M M
MM
Sztaricskai
F
F
Dobrynin
Y V
YV
Nikolaeva
T G
TG
D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis* / Q000494:pharmacology; D002360:Carubicin / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D003630:Daunorubicin / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D010752:Phosphoramide Mustards / Q000138:chemical synthesis* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D018906:Antineoplastic Agents, Alkylating; D010752:Phosphoramide Mustards; D002360:Carubicin; D003630:Daunorubicin