Research on Anti-Tumor Active Site of Marine Source Compound, Halichondrin

海洋源化合物软海绵素抗肿瘤活性位点研究

• 批准号: 10671995
• 负责人: HORITA Kiyoshi
• 金额: $ 2.18万
• 依托单位: Health Sciences University of Hokkaido
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 1998
• 资助国家: 日本
• 起止时间: 1998 至 2000
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-10671995/
• 关键词: polyether; macrolactone; halichondrin B; cytotoxity; KB cell; L1210 cell; ポリエーテル; 殺細胞活性; マクロラクトン部分; 分子内 Michael反応

We succeeded in establishing a flexible and efficient synthetic pathway of macrolactone part and the polyether part of the highly strong antitumor polyether macrolide, halichondrin B, isolated from cheap and commercially available starting materials. Two compounds, a part of polyether unit, in our synthetic intermediates were compared by cytotoxity against KB and L1210 in vitro . It found that the polyether unit indicated considerably strong cytotoxity for the first time although the activities of the two examined compounds were not so high as those of the natural halichondrin B.

我们成功地建立了一个灵活的和有效的合成途径的大环内酯部分和聚醚部分的高度强大的抗肿瘤聚醚大环内酯，软海绵素B，从廉价和商业上可获得的起始原料分离。比较了我们合成中间体中的两种化合物（聚醚单元的一部分）对KB和L1210的体外细胞毒性。结果表明，尽管两个化合物的活性不如天然软海绵素B，但首次发现聚醚单元具有较强的细胞毒性。

项目成果

Horita, K., Nishibe, S., Yonemitsu, O.: "Research on Anti-Tumor Active Site of Marine Source Compound, Halichondrin B"New Trends and Methods in Natural Products' Research. 176-183 (1999)

Horita, K.、Nishibe, S.、Yonemitsu, O.：“海洋源化合物软海绵素 B 的抗肿瘤活性位点研究”天然产物研究的新趋势和新方法。

Horita, K., Sakurai, Y., Nagasawa, M., Yonemitsu, O.: "Synthetic Studies of Halichondrin B, an Antitumor Polyether Macrolide Isolated from a Marine Sponge.9."Chem.Pharm.Bull.. 46(8). 1199-1216 (1998)

Horita, K.、Sakurai, Y.、Nagasawa, M.、Yonemitsu, O.：“软海绵素 B 的合成研究，一种从海洋海绵中分离出的抗肿瘤聚醚大环内酯。9。”Chem.Pharm.Bull.. 46(8

Sardari, S., Nishibe, S., Horita, K., Nikaido, T.and Daneshtalab, M.: "Semisynthesis of Antifungal Flavonoids from Ledum palustre subsp decunbens."Pharmazie.. 54(7). 554-556 (1999)

Sardari, S.、Nishibe, S.、Horita, K.、Nikaido, T. 和 Daneshtalab, M.：“来自杜香亚种 decunbens 的抗真菌类黄酮的半合成”。Pharmazie.. 54(7)。

Sardari, S., Mori, Y., Horita, K., Micetich, R.G., Nishibe, S.and Daneshtalab, M.: "Synthesis and Antifungal Activity of Coumarins and Angular Furanocoumarins"Bioorg.Wed.Chem.. 7. 554-556 (1999)

Sardari, S.、Mori, Y.、Horita, K.、Micetich, R.G.、Nishibe, S. 和 Daneshtalab, M.：“香豆素和角呋喃香豆素的合成和抗真菌活性”Bioorg.Wed.Chem.. 7. 554

Horita K.: "Synthetic Study of a Highly Antitumorigenic Marine Phytochemical Halichondrin B"Phytochemicals and Phytopharmaceuticals. 35. 386-397 (2000)

Horita K.：“高度抗肿瘤海洋植物化学物质软海绵素 B 的合成研究”植物化学物质和植物药物。