著者
Takeo KAWAGUCHI Masahiko SAITO Mineo SANEYOSHI
出版者
The Japanese Cancer Association
雑誌
Japanese Journal of Cancer Research GANN (ISSN:09105050)
巻号頁・発行日
vol.77, no.5, pp.436-439, 1986 (Released:2008-03-17)
参考文献数
13

The antitumor effect of 5-fluoro-2'-deoxy-uridine (FUdR) esters on L1210 in mice was enhanced by the simultaneous po administration of FUdR esters and acyclothymidine [5-methyl-1-(2'-hydroxyethoxymethyl)uracil]-esters. Acyclothymidine (AcTdR), which strongly inhibits the phospholytic degradation of FUdR, was released from the AcTdR esters by enzymatic hydrolysis. The FUdR esters and AcTdR esters were found to be compatible in terms of their physicochemical properties and susceptibility to enzymatic hydrolysis.
著者
MINEO SANEYOSHI MOTOKO INOMATA TERUAKI SEKINE AKIO HOSHI FUMIKO FUKUOKA
出版者
The Pharmaceutical Society of Japan
雑誌
Journal of Pharmacobio-Dynamics (ISSN:0386846X)
巻号頁・発行日
vol.1, no.3, pp.168-174, 1978 (Released:2008-02-21)
参考文献数
12
被引用文献数
6 6

Reaction of S-benzylthioisothiouronium hydrochloride with 6-mercaptopurine (1), 9-β-D-ribofuranosyl-6-mercaptopurine (2), 6-thioguanine (3) and 9-β-D-ribofuranosyl-6-thioguanine (4) afforded corresponding benzyl disulfide derivatives (5-8) in good yield. These compounds were converted easily to parent mercapto derivatives when they were treated with various reducing agents such as β-mercaptoethanol. Antitumor activity of compound 5 was higher than that of 1 both in ascites Sarcoma 180 and in Nakahara-Fukuoka sarcoma systems. However, toxicity and immunosuppressive activity of compound 5 and 6 were higher than those of 1 and 2, respectively.
著者
吉田 光二 星 昭夫 / 実吉 峯郎 MINEO SANEYOSHI
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.30, no.3, pp.1018-1023, 1982-03-25 (Released:2008-03-31)
参考文献数
23
被引用文献数
4 5

The mode of antiproliferative action of two 5-fluorocytosine nucleosides, 5-fluoro-cytidine (FCR) and 5-fluoro-2'-deoxycytidine (FCdR), was examined using mouse leukemia L5178Y cells in vitro. FCR and FCdR were markedly active against L5178Y cells, though the cells were deficient in cytidine deaminase activity. Both compounds increased the incorporation of 14C-labeled thymidine into the acid-insoluble fraction of L5178Y cells and decreased labeled deoxycytidine incorporation. In reversal studies, the antiproliferative effects of both compounds were almost abolished by simultaneous addition of thymidine or deoxyuridine. Deoxycytidine completely reversed the growth inhibition caused by FCdR, but not that caused by FCR. These results demonstrate that the cytotoxicity of both compounds is due to inhibition of thymidylate synthetase, presumably through formation of 5-fluoro-2'-deoxyuridine monophosphate (FdUMP) after deamination by deoxycytidylate deaminase in the pyrimidine de novo pathway.
著者
MITSUAKI MAEDA MINEO SANEYOSHI YUTAKA KAWAZOE
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.19, no.8, pp.1641-1649, 1971-08-25 (Released:2011-02-08)
参考文献数
28
被引用文献数
14 21

The reaction mechanism for the hydrogen exchange of C-8 hydrogens of purine ribosides was discussed on the basis of the pD-rate profiles and the effect of 6-substituents on the rate. It was shown that the rate depended on concentrations of the purine and D2O and that the observed second-order rate constant was expressed as kOD-KD2O/Ka (N7) where kOD-was the rate constant for hydrogen exchange of N7-protonated purines by attack with the OD-, KD2O was the dissociation constant of D2O, and Ka (N7) was the dissociation constant of N7-protonated purines.