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Ferricenium complexes: A new type of water-soluble antitumor agent
Journal of Cancer Research and Clinical Oncology ( IF 2.7 ) Pub Date : 1984-11-01 , DOI: 10.1007/bf00390468 P. K�pf-Maier , H. K�pf , E. W. Neuse
Journal of Cancer Research and Clinical Oncology ( IF 2.7 ) Pub Date : 1984-11-01 , DOI: 10.1007/bf00390468 P. K�pf-Maier , H. K�pf , E. W. Neuse
SummaryThe antitumor activity of a series of iron complexes, i.e., of ferrocene [Cp2Fe], of tetrachloroferrates(III) [R4N]+[FeCl4]-, and of ferricenium complexes [Cp2Fe]+X- (X-=[FeCl4]-, 1/2[Cl3FeOFeCl3]2-, [H5Mo7O24]-·2H2O, [2,4,6-(NO2)3C6H2O]-, or [CCl3COO]-·2 CCl3COOH) was investigated against EAT in CF1 mice. Whereas ferrocene and the ammonium tetrachloroferrates(III) did not show recognizable tumor-inhibiting activity, such activity was exhibited by the water-soluble, salt-like ferricenium complexes; the best antineoplastic properties, with optimum cure rates of 100%, were found for ferricenium picrate and ferricenium trichloroacetate.The ferricenium compounds are the first iron complexes for which antineoplastic activity has now been shown. They represent a new type of antitumor agent insofar as they differ fundamentally from known inorganic and organometallic antitumor agents (a) by their ionic, salt-like character, which is responsible for their high water solubility, and (b) by the absence of a cis-dihalometal moiety; this moiety has been recognized as important for the intracellular action of other known inorganic cytostatics.
中文翻译:
铁络合物:一种新型水溶性抗肿瘤剂
总结一系列铁配合物的抗肿瘤活性,即二茂铁[Cp2Fe]、四氯铁酸盐(III) [R4N]+[FeCl4]-和三价铁配合物[Cp2Fe]+X-(X-=[FeCl4]-) , 1/2[Cl3FeOFeCl3]2-, [H5Mo7O24]-·2H2O, [2,4,6-(NO2)3C6H2O]-, 或 [CCl3COO]-·2CCl3COOH) 在 CF1 小鼠中对 EAT 进行了研究。虽然二茂铁和四氯铁酸铵 (III) 没有表现出可识别的肿瘤抑制活性,但水溶性、盐状铁络合物显示出这种活性;苦味酸铁和三氯乙酸铁具有最佳的抗肿瘤特性,最佳治愈率为 100%。铁化合物是目前已显示出抗肿瘤活性的第一种铁络合物。它们代表了一种新型的抗肿瘤剂,因为它们与已知的无机和有机金属抗肿瘤剂有着根本的不同(a)它们的离子、盐样特性,这是它们高水溶性的原因,以及(b)不存在顺式二卤金属部分;该部分已被认为对其他已知无机细胞抑制剂的细胞内作用很重要。
更新日期:1984-11-01
中文翻译:
铁络合物:一种新型水溶性抗肿瘤剂
总结一系列铁配合物的抗肿瘤活性,即二茂铁[Cp2Fe]、四氯铁酸盐(III) [R4N]+[FeCl4]-和三价铁配合物[Cp2Fe]+X-(X-=[FeCl4]-) , 1/2[Cl3FeOFeCl3]2-, [H5Mo7O24]-·2H2O, [2,4,6-(NO2)3C6H2O]-, 或 [CCl3COO]-·2CCl3COOH) 在 CF1 小鼠中对 EAT 进行了研究。虽然二茂铁和四氯铁酸铵 (III) 没有表现出可识别的肿瘤抑制活性,但水溶性、盐状铁络合物显示出这种活性;苦味酸铁和三氯乙酸铁具有最佳的抗肿瘤特性,最佳治愈率为 100%。铁化合物是目前已显示出抗肿瘤活性的第一种铁络合物。它们代表了一种新型的抗肿瘤剂,因为它们与已知的无机和有机金属抗肿瘤剂有着根本的不同(a)它们的离子、盐样特性,这是它们高水溶性的原因,以及(b)不存在顺式二卤金属部分;该部分已被认为对其他已知无机细胞抑制剂的细胞内作用很重要。