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Application of plant allylpolyalkoxybenzenes in synthesis of antimitotic phenstatin analogues |
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| Authors: | Titov Ilia Y Sagamanova Irina K Gritsenko Roman T Karmanova Irina B Atamanenko Olga P Semenova Marina N Semenov Victor V |
| Institution: | a Zelinsky Institute of Organic Chemistry RAS, 47 Leninsky Prospect, 119991 Moscow, Russia b Chemical Block Ltd, 3 Kyriacou Matsi, 3723 Limassol, Cyprus c Institute of Developmental Biology RAS, 26 Vavilov Str., 119334 Moscow, Russia |
| Abstract: | 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. |
| Keywords: | VYSWLFFVXPILFF-UHFFFAOYSA-N |
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