Synthesis, characterization and in vitro antiproliferative activities of new 13-cis-retinoyl ferrocene derivatives
Synthesis, characterization and in vitro antiproliferative activities of new 13-cis-retinoyl ferrocene derivatives
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DOI：
10.1016/j.ejmech.2009.01.029
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发表时间：
2009-06-01
影响因子：
6.7
通讯作者：
Xiang, Jiannan
中科院分区：
文献类型：
--
作者：
Long, Bohua;Liang, Shengzong;Xiang, Jiannan
为了改善视黄酰基衍生物的生物活性，采用改进的Suzuki交叉偶联法合成了单芳基二茂铁基醇9a和9 b，并通过Mitsunobu反应以中等至良好的产率合成了它们的13-顺式视黄酸类似物。其结构经IR、~ 1H NMR、（CNMR）-C ~（13）、MS和元素分析确证，并测定了其体外抗肿瘤活性。生物活性测定结果表明，这些有机金属类似物的抗增殖活性高于母体13-顺式维甲酸和其他维甲酸衍生物。(C)2009年Elsevier Masson SAS。All rights reserved.
in order to improve biological behavior of the retinoyl derivatives, monoarylferrocenyl alcohols 9a and 9b were synthesized by an improved Suzuki cross-coupling method and their 13-cis-retinoic acid analogues were prepared in moderate to good yields via the Mitsunobu reaction. Their structures were confirmed by IR, H-1 NMR, (CNMR)-C-13, MS spectra and element analysis and their antiproliferative activities were determined in vitro using human cancer cell lines. The results of bioassay showed that these organometallic analogues exhibited higher antiproliferative activities than parent 13-cis-retinoic acid and other retinoyl derivatives. (C) 2009 Elsevier Masson SAS. All rights reserved.