- 著者
- Hiroyuki Hayakawa Hiromichi Tanaka Naoko Itoh Masako Nakajima Tadashi Miyasaka Kentaro Yamaguchi Yoichi Iitaka
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.35, no.6, pp.2605-2608, 1987-06-25 (Released:2009-10-19)
- 参考文献数
- 26
- 被引用文献数
- 30 43
The reaction of organolithium, Grignard, and organoaluminum reagents with 2'- and 3'-ketouridine derivatives was examined. For the reaction of 2', 5'-bis-0- (tert-butyldimethylsilyl) -3'-ketouridine, both organolithiums and organoaluminums seem to be practically useful. But only organoaluminums gave satisfactory yields in the reaction of 3', 5'-0- (tetraisopropyldisiloxan-1, 3-diyl) -2'-ketouridine.
- 著者
- MASAHIRO SUZUKI HIROMICHI TANAKA TADASHI MIYASAKA
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.35, no.10, pp.4056-4063, 1987-10-25 (Released:2009-10-19)
- 参考文献数
- 14
- 被引用文献数
- 4 12
Several 5-carbon-substituted 1-β-D-ribofuranosylimidazole-4-carboxamides were synthesized via the direct C-5 lithiation of a protected 4-carboxamide derivative as the key reaction step. Wittig reaction of a 5-formyl derivative was also examined.
1 0 0 0 OA ANTITUMOR ACTIVITY OF A NEW CAMPTOTHECIN DERIVATIVE, SN-22, AGAINST VARIOUS MURINE TUMORS
- 著者
- TAKEHIKO KUNIMOTO KAZUO NITTA TOMIKO TANAKA NOBUAKI UEHARA HIROYASU BABA MIEKO TAKEUCHI TERUO YOKOKURA SEIGO SAWADA TADASHI MIYASAKA MASAHIKO MUTAI
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Journal of Pharmacobio-Dynamics (ISSN:0386846X)
- 巻号頁・発行日
- vol.10, no.3, pp.148-151, 1987 (Released:2008-02-19)
- 参考文献数
- 7
- 被引用文献数
- 7 15
The antitumor activity of a new camptothecin derivative, SN-22, was evaluated by using various murine tumors. SN-22 showed strong activity against the ascites tumors Ehrlich carcinoma, MM46, CCM, L1210, L5178Y, P388, Meth A, and B16 melanoma. In particular, the maximum increase in life span values for Ehrlich, MM46 and CCM were as high as 253-606% and many mice were cured of these tumors. The effect of SN-22 against solid tumors was also determined. The inhibition ratios were higher than 70% for MM46 and L5178Y. The LD50 of SN-22 in ICR mice was about 1.5 times that of the parent camptothecin.
- 著者
- HIROYUKI HAYAKAWA KAZUHIRO HARAGUCHI HIROMICHI TANAKA TADASHI MIYASAKA
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.35, no.1, pp.72-79, 1987-01-25 (Released:2009-10-19)
- 参考文献数
- 16
- 被引用文献数
- 29 43
The sugar moiety of adenosine, inosine, or guanosine was protected with a tert-butyldimethylsilyl group. The C-8 lithiation of these protected nucleosides was carried out with lithium diisopropylamide in tetrahydrofuran at below -70°C. The reactions of the C-8-lithiated species with MeI, HCO2Me, and ClCO2Me were examined. The resulting products having a carbon substituent at the C-8 position were converted to the corresponding 8-carbon-substituted purine nucleosides by treatment with tetrabutylammonium fluoride. The whole sequence constitutes a simple method for the preparation of 8-carbon-substituted purine nucleosides from intact purine nucleosides.