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    • 1. 发明授权
    • Halimide, a cytotoxic marine natural product, and derivatives thereof
    • Halimide,细胞毒性海洋天然产物及其衍生物
    • US6069146A
    • 2000-05-30
    • US191475
    • 1998-11-12
    • William FenicalPaul R. JensenXing C. Cheng
    • William FenicalPaul R. JensenXing C. Cheng
    • A61K31/497A61P35/00C07D403/06A61K31/496
    • C07D403/06A61K31/497
    • The present invention provides a substantially purified compound having the structure: ##STR1## wherein R.sub.1 to R.sub.9 are defined; or a salt of the compound, and provides pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier. The invention also provides methods of reducing or inhibiting mitosis of a cell by contacting the cell with a compound of the invention, which blocks the cell at the G2/M phase of the cell cycle. The invention also provides a method of reducing the severity of a pathology characterized, at least in part, by undesirable proliferation of a population of cells in a subject by administering to the subject a compound of the invention in an amount sufficient to reduce or inhibit proliferation of the population of cells.
    • 本发明提供了具有以下结构的基本上纯化的化合物:其中R1至R9被定义; 或化合物的盐,并提供包含本发明化合物和药学上可接受的载体的药物组合物。 本发明还提供了通过使细胞与本发明的化合物接触来减少或抑制细胞有丝分裂的方法,该化合物在细胞周期的G2 / M期阻断细胞。 本发明还提供了一种降低病症严重性的方法,所述方法至少部分地由受试者中细胞群的不期望的增殖表达,所述方法通过向受试者施用足以减少或抑制增殖的量的本发明化合物 的细胞群体。