de Lima Dênis Pires, Rotta Rodrigo, Beatriz Adilson, Marques Maria Rita, Montenegro Raquel C, Vasconcellos Marne C, Pessoa Cláudia, de Moraes Manoel O, Costa-Lotufo Letícia V, Frankland Sawaya Alexandra Christine Helena, Eberlin Marcos Nogueira
Departamento de Química, Universidade Federal de Mato Grosso do Sul, CP 549, 79070-900 Campo Grande, MS, Brazil.
Eur J Med Chem. 2009 Feb;44(2):701-7. doi: 10.1016/j.ejmech.2008.05.003. Epub 2008 May 15.
This work deals with the preparation of stilbene-based resveratrol analogs by employing the Perkin reaction, aiming at synthesizing potential antitumor lead compounds and evaluating their pharmacological activities. The proliferation inhibitor test against tumor cell lines identified analogs 9 and 11 as the most active among all synthesized derivatives, presenting IC(50) in micromolar range for certain cell lines. For study on the embryonic development, compounds 8 and 9 at the lowest tested concentration (41.7 microM) that inhibited sea urchin egg development, but only after third cleavage were used. Both the compounds inhibited 100% of normal development since first cleavage. These data partially corroborated the results obtained with MTT assay using tumor cell lines. None of the tested compounds revealed hemolytic action in assay with mouse erythrocytes.
这项工作通过珀金反应制备基于芪的白藜芦醇类似物，旨在合成潜在的抗肿瘤先导化合物并评估其药理活性。针对肿瘤细胞系的增殖抑制试验确定类似物9和11是所有合成衍生物中活性最高的，对某些细胞系呈现出微摩尔范围内的半数抑制浓度（IC50）。为了研究胚胎发育，使用了化合物8和9，它们在最低测试浓度（41.7微摩尔）下抑制海胆卵发育，但仅在第三次卵裂后才起作用。这两种化合物自第一次卵裂起就抑制了100%的正常发育。这些数据部分证实了使用肿瘤细胞系进行MTT试验所获得的结果。在所测试的化合物中，没有一种在小鼠红细胞试验中显示出溶血作用。
