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    • 3. 发明申请
    • SUBSTITUTED STILBENES AND THEIR REACTIONS
    • 取代的STILBENES及其反应
    • WO02050007A2
    • 2002-06-27
    • PCT/GB2001/005702
    • 2001-12-20
    • A61P35/00C07C43/215C07C43/23C07C46/06C07C50/30C07C205/35C07C205/37C07C205/44C07C271/22C07D213/68C07F7/18A61K31/09A61K31/12A61K31/215A61K31/27A61K31/44C07C50/28
    • C07F7/1852C07C43/215C07C43/23C07C46/06C07C50/30C07C205/35C07C205/37C07C205/44C07C271/22C07D213/68
    • The present invention relates to stilbene and quinone compounds related to combretastatin A-4 and their use as anticancer compounds and prodrugs. The compounds include those with an alkyl group on the double bond of cis or trans-stilbenes, compounds with one or more (and preferably 2 or 3) alkyl group substituents on the stilbene A ring, compounds with an alkoxy group other than methoxy at position 3, 4, and/or 5 of the stilbene A ring, compounds (or prodrugs) in which BOC amino acid esters are formed with the phenolic hydroxyl at the 3-position of the B ring and compounds (or prodrugs) based on a benzoquinone B ring. The present invention further relates to the photochemical reactions of stilbene compounds, either the above compounds disclosed for the first time herein or compounds based on prior art stilbenes. These reactions include the photochemical release of an active form of the compound from a prodrug conjugate and the photochemical isomerisation of the compounds, especially from a trans to cis form of compounds. The reactions can be used alone or in combination to convert inactive or comparatively less active forms of the compounds to more active forms,thereby allowing the compounds to be selectively targeted, e.g. activating them at the site of a tumour.
    • 本发明涉及与考布他汀A-4相关的芪和醌化合物及其作为抗癌化合物和前药的用途。 化合物包括在顺式或反式二苯乙烯的双键上具有烷基的化合物,在二苯乙烯A环上具有一个或多个(优选2或3个)烷基取代基的化合物,位置以外的甲氧基的烷氧基的化合物 3,4或5,其中BOC氨基酸酯与B环3位上的酚羟基形成的化合物(或前药)和基于苯醌的化合物(或前药) B戒指 本发明还涉及二苯乙烯化合物的光化学反应,上述化合物是本文首次公开的化合物或基于现有技术的二苯乙烯的化合物。 这些反应包括来自前药缀合物的化合物的活性形式的光化学释放和化合物的光化学异构化,特别是从反式到顺式形式的化合物。 反应可以单独使用或组合使用以将化合物的无活性或相对较少活性的形式转化为更具活性的形式,从而允许化合物选择性靶向。 在肿瘤部位激活它们。