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抗肿瘤金属茂:新进展与毒理学特征

Antitumor metallocenes: new developments and toxicologic features.

作者信息

Köpf-Maier P, Köpf H

出版信息

Anticancer Res. 1986 Mar-Apr;6(2):227-33.

PMID:3707060
Abstract

Recent results concerning new antitumor metallocene derivatives have shown that not only numerous titanocene dihalides and bis(pseudohalides) exhibit antiproliferative activity, but that also some titanocene complexes (C5H5)2TiX2 containing carboxylates or hydrochlorinated aminothiophenolates as ligands X, are characterized by pronounced antineoplastic efficacy. Whereas antitumor activity of metallocene derivatives has originally been established against Ehrlich ascites tumor, recent experimental results demonstrate antiproliferative activity also against B16 melanoma, sarcoma 180, as well as against human tumors heterotransplanted to athymic mice. Studies upon the organ toxicity of titanocene dichloride indicate a pattern of toxicity markedly differing from that observed after treatment with cytostatic platinum compounds.

摘要

有关新型抗肿瘤茂金属衍生物的最新研究结果表明,不仅众多二卤代钛茂和双(拟卤化物)表现出抗增殖活性,而且一些以羧酸盐或氢氯化氨基硫酚盐作为配体X的钛茂配合物(C5H5)2TiX2也具有显著的抗肿瘤功效。虽然茂金属衍生物的抗肿瘤活性最初是针对艾氏腹水瘤确定的,但最近的实验结果表明,其对B16黑色素瘤、肉瘤180以及移植到无胸腺小鼠体内的人类肿瘤也具有抗增殖活性。对二氯钛茂的器官毒性研究表明,其毒性模式与使用细胞抑制性铂化合物治疗后观察到的毒性模式明显不同。

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