Isolation and structure of hallistatin 2

C - Chemistry – Metallurgy – 07 – H

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C07H 19/01 (2006.01) A61K 31/70 (2006.01) C07D 493/22 (2006.01) C07H 9/02 (2006.01) C12P 17/18 (2006.01) C12P 19/44 (2006.01)

Patent

CA 2113657

ABSTRACT OF THE DISCLOSURE An intensive long-term investigation of marine organisms as sources of new anticancer drugs has led to the isolation and structural elucidation (primarily by high field NMR and mass spectrometry) of halistatin 2, a new polyether macrolide of the halipyran-type, from the Western Indian Ocean sponge Axinella cf. carteri (Dendy). Halistatin 2 (1.4 x 10-6% yield) caused the accumulation of cells arrested in mitosis, inhibited tubulin polymerization, and inhibited the binding of radiolabeled vinblastine and GTP to tubulin. Further, Halistatin 2 displayed significant activity against selected human tumor cell lines.

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