Application of plant allylpolyalkoxybenzenes in synthesis of antimitotic phenstatin analogues

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• 作者：Ilia Y. Titovp>ap>p> ; p>p>il_tit@bk.rup> ; Irina K. Sagamanovap>ap>p> ; p>p>sagamanova@mail.rup> ; Roman T. Gritsenkop>ap>p> ; p>p>romagree@gmail.comp> ; Irina B. Karmanovap>ap>p> ; p>p>info@chemblock.comp> ; Olga P. Atamanenkop>ap>p> ; p>p>info@chemblock.comp> ; Marina N. Semenovap>bp>p> ; p>p>cp>p> ; p>p>ms@chemical-block.comp> ; Victor V. Semenovp>ap>p> ; p>p>cp>p> ; p>p>vs@zelinsky.rup>
• 关键词：Allylpolyalkoxybenzenes ; Antimitotic agents ; Phenstatin ; Tubulin ; Sea urchin embryo
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 March 2011
• 年：2011
• 卷：21
• 期：6
• 页码：1578-1581
• 全文大小：281 K

文摘

Phenstatin and its derivatives with the modified ring A have been synthesized, using plant allylpolyalkoxybenzenes as a starting material. The targeted molecules were evaluated in a phenotypic sea urchin embryo assay for antiproliferative activity. It was found that phenstatin ring A modifications yielded antimitotic compounds. The most effective myristicin derivative 7d (combretastatin A-2 analogue) was determined to be ca. 10 times more potent than phenstatin, displaying antimitotic tubulin-destabilizing activity at the same concentration range as combretastatins. In contrast to combretastatins, 7d featured the steric stability with potential for further design as anticancer agent.