Cytostatic activity in vitro of some new cyclophosphazene oligomers.
Cytostatic activity of newly synthesized aziridinyl substituted cyclophosphazenes was tested in two in vitro systems. First, the compounds were tested by total cell protein inhibition test on human KB tumor cell line. Selected active compounds were tested in a clonogenic assay on murine L1210 leukemia cells. Out of 18 compounds tested, 12 were newly synthesized, 3 were their substrates and 4 were compounds with known cytostatic activity, used as a positive controls. Four of the newly synthesized compounds, designated with symbols: BANF-4Az, BBNF-4Az. T-oFDA-Az and W-10 revealed cytostatic activity for KB cells (ED50 = 3.4-19 micrograms/mL) and were tested in clonogenic assay. One of these compounds, namely T-oFDA-Az was subsequently selected for the further steps of screening for antitumor activity in animal tumor models.
Duś
D
D
Department of Tumor Immunology, Polish Academy of Sciences, Wrocław.
Brandt
K
K
Wojdat
E
E
Gebarowska
E
E
Jedliński
Z
Z
Radzikowski
C
C
D000477:Alkylating Agents / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry; D001388:Aziridines / Q000737:chemistry / Q000494:pharmacology*; D003114:Colony-Forming Units Assay; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007939:Leukemia L1210 / Q000188:drug therapy; D009943:Organophosphorus Compounds / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000477:Alkylating Agents; D000970:Antineoplastic Agents; D001388:Aziridines; D009943:Organophosphorus Compounds