The interaction of chalcones with tubulin.

Anti-cancer drug design Pub Date : 2000-04-01
N J Lawrence, A T McGown, S Ducki, J A Hadfield
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Abstract

The chalcone 3,4,3',4',5'-pentamethoxychalcone is a potent cytotoxic agent. A series of chalcones and (E)-4-(4'-hydroxyphenyl)but-3-en-2-one were prepared and assessed for their ability to inhibit cell growth in vitro. The cytotoxicity correlates with their ability to bind to tubulin as measured by immunofluorescence, cell cycle analysis and disruption of microtubule assembly. Some of the chalcones were shown to bind to the type II oestrogen receptor.

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查尔酮与微管蛋白的相互作用。
查尔酮3,4,3',4',5'-五甲基查尔酮是一种有效的细胞毒性物质。制备了一系列查尔酮和(E)-4-(4′-羟基苯基)- 3-烯-2-酮,并对其体外抑制细胞生长的能力进行了评价。细胞毒性与它们与微管蛋白结合的能力相关,通过免疫荧光、细胞周期分析和微管组装的破坏来测量。一些查尔酮被证明与II型雌激素受体结合。
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