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Antitumor activity of 1 M tegafur-0.4 M 5-chloro-2,4-dihydroxypyridine-1 M potassium oxonate (S-1) against human colon carcinoma orthotopically implanted into nude rats.
It is suggested that this orthotopic human colorectal tumor model in nude rats is useful to evaluate the clinical therapeutic efficacy of drugs or therapies for coloretectal cancer, and that S-1 had a higher therapeutic effect on human colorescent tumor than UFT did.
Antitumor activity and low intestinal toxicity of S-1, a new formulation of oral tegafur, in experimental tumor models in rats
The results suggest that CDHP, which is a potent inhibitor of 5-FU degradation, increases the antitumor activity of FT, and that Oxo, who is an inhibitor of5-FU phosphorylation, locally protects the gastrointestinal tract from 5-fluorouracil-induced toxicity without decreasing the antitUMor activity.
Preclinical antitumor efficacy of S-1: a new oral formulation of 5-fluorouracil on human tumor xenografts.
The results of this study suggested that based on its biological and pharmacokinetic characteristics, oral S-1 should be active against various human cancers.
Antitumor agents. I. DNA topoisomerase II inhibitory activity and the structural relationship of podophyllotoxin derivatives as antitumor agents.
The results of antitumor test in mice bearing L 1210 on podophyllotoxin derivatives suggest the following: 1) the strong cytotoxic effect itself is not a good indication of antitUMor activity in vivo as long as it is associated with inhibition of tubulin polymerization.
Pretreatment with S-1, an oral derivative of 5-fluorouracil, enhances gemcitabine effects in pancreatic cancer xenografts.
The GEM/S-1 combination therapy in patients with pancreatic cancer may be promising and should be tested in clinical trials, based on the effects of S-1 on the uptake of GEM.
[Prolongation of survival and antitumor activity of antitumor drugs in murine cancer cachexia model].
It is shown that UFT can prolong the survival period due to improvement of cancer cachexia and prolongs life by decreased IL-6 resulting from decreased PGE2, and plasma interleukin-6 (IL-6) was measured and found that U FT-administration lowered the plasma IL- 6 level more than other drugs.
New antifungal 1,2,4-triazoles with difluoro(substituted sulfonyl)methyl moiety.
New 1,2,4-triazoles (2) having a difluoro(substituted sulfonyl)methyl moiety were designed and synthesized via alpha,alpha-difluoro-alpha-(substituted thio)acetophenones (3). Compounds (2) showed
Effect of 1,3,3,5,5-pentaziridino-1-thia-2,4,6-triaza-3,5-diphosphorine-1-oxide, a new antitumor agent with inorganic ring, on various experimental tumors.
SOAz was active against B16 melanoma and Meth A, and demonstrated high activity against a subline of L1210 leukemia resistant to cyclophosphamide, and exhibited 80-100% inhibition of tumor local growth in all of four experimental tumor systems used in the present study.
Terpenoids. LIII. Antitumor activity of trichorabdals and related compounds.
Among the three types, enmein-, oridonin-, and trichorabdal-type, of diterpenoids from Rabdosia trichocarpa, the latter showed the highest antitumor activity against Ehrlich ascites carcinoma in mice, attributed to synergistic increase arising from the presence of two active sites in one molecule.