Unsaturated genistein disaccharide glycoside as a novel agent affecting microtubules
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- 作者：Aleks ; ra Rusin ; Agnieszka Gogler ; Magdalena Gł ; owala-Kosiń ; ska ; Daria Bochenek ; Aleks ; ra Gruca ; Grzegorz Grynkiewicz ; Jadwiga Zawisza ; Wiesł ; aw Szeja ; Zdzisł ; aw Krawczyk
- 关键词：Genistein glycoside ; Microtubule interfering drugs
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 September 2009
- 年：2009
- 卷：19
- 期：17
- 页码：4939-4943
- 全文大小：602 K
文摘
Genistein, due to its recognized chemopreventive and antitumor potential, is a molecule of interest as a lead compound in drug design. While multiple molecular targets for genistein have been identified, so far neither for this isoflavonoid nor for its natural or synthetic derivatives disruption of microtubules and mitotic spindles has been reported. Here we describe such properties of the synthetic glycosidic derivative of genistein significantly more cytotoxic than genistein, 7-O-(2,3,4,6-tetra-O-acetyl-β-d-galactopyranosyl)-(1→4)-(6-O-acetyl-hex-2-ene-α-d-erythro-pyranosyl)genistein, shortly named G21. We found that G21 causes significant mitotic delay, frequent appearance of multipolar spindles, and alteration of the interphase microtubule array.