ECB-ART-41926
Bioorg Med Chem Lett
2011 Mar 15;216:1578-81. doi: 10.1016/j.bmcl.2011.01.124.
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Application of plant allylpolyalkoxybenzenes in synthesis of antimitotic phenstatin analogues.
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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.
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Genes referenced: LOC100887844 tubgcp2