Title:
HALISTATIN 2
Document Type and Number:
Japanese Patent JP3430317
Kind Code:
B2
Abstract:
PURPOSE: To provide halistatin 2 which exerts, as an anti-tumor agent, a particularly excellent activity against leukemia, small cell carcinoma of lung, large bowel cancer, CNS cancer and melanoma.
CONSTITUTION: The halistatin 2 is shown by the formula. It is extracted with methanol-dichloromethane from the sponge Axinella-cartain 2 from the west Indian Ocean and distributed between hexane-dichloromethane. It is obtained with a yield of 1.4×10-6% and causes the accumulation of cells arrested in mitosis, inhibits tubulin polymerization, and inhibits the binding of radiolabeled vinblastin and GTP to tubulin, and exerts effective activity against human tumor cells. The IR spectrum of halistatin 2 has adsorption of 3358, 1734 and 1653 cm-1 respectively corresponding to an OH group, ester carbonyl and a double bond, and FABMS has a peak of m/z 1145 [M+Li]+ corresponding to a theoretical m. wt. of 1138, thus its molecular formula is C61H86O20.
Inventors:
George Earl Pettit
Feng Gao
Feng Gao
Application Number:
JP3076094A
Publication Date:
July 28, 2003
Filing Date:
January 17, 1994
Export Citation:
Assignee:
Arizona Board of Regents
International Classes:
A61K31/365; A61K35/56; A61P35/00; A61P35/02; C07D493/22; C07H9/02; C12P17/18; C12P19/44; (IPC1-7): C07D493/22; A61K31/365; A61P35/00; A61P35/02
Other References:
Ｊ．Ｍｅｄ．Ｃｈｅｍ．，Ｖｏｌ．３４（１９９１）Ｐ．３３３９−３３４０
Ｐｕｒｅ．＆ Ａｐｐｌ．Ｃｈｅｍ．，Ｖｏｌ．５８，Ｎｏ．５（１９８６年）Ｐ．７０１−７１０
Ｐｕｒｅ．＆ Ａｐｐｌ．Ｃｈｅｍ．，Ｖｏｌ．５８，Ｎｏ．５（１９８６年）Ｐ．７０１−７１０
Attorney, Agent or Firm:
Hisao Kuwahara