Anti-tumor effect of dithiole compounds.
A series of dithiole compounds, N-(1,3-dithiole-2-ylidene)-N,N-dialkyl-ammonium salts, was synthesized and tested for anti-tumor activity. Most of them exhibited a potent cytotoxic activity against cultured cells at IC50 concentrations less than 1 micrograms/ml. They were also effective in increasing the life-span of mice bearing L1210 leukemic cells. Their anti-tumor activities both in vitro and in vivo were related to the length of alkyl chain moieties, among which EX-015, having n-decyl chains, was found to be most effective in vivo; EX-015 prolonged the survival time of mice implanted with L1210 cells by 69% when given once daily for 5 days at 0.8 mg/kg. In addition, EX-015 inhibited the RNA and protein syntheses of L1210 cells, but less so with the DNA synthesis.
Yoshida
E
E
Exploratory Research Laboratories, Banyu Pharmaceutical Co., Ltd, Tokyo, Japan.
Fukami
T
T
Takamiya
K
K
Okura
A
A
D000818:Animals; D000970:Antineoplastic Agents; D004353:Drug Evaluation, Preclinical; D005260:Female; D007939:Leukemia L1210 / Q000378:metabolism / Q000473:pathology; D051379:Mice; D008815:Mice, Inbred Strains; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000494:pharmacology*; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D013438:Sulfhydryl Compounds