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二茂钛配合物的肿瘤抑制作用。对B16黑色素瘤和结肠38癌的活性。

Tumor inhibition by titanocene complexes. Activity against B16 melanoma and colon 38 carcinoma.

作者信息

Köpf-Maier P, Köpf H

出版信息

Arzneimittelforschung. 1987 May;37(5):532-4.

PMID:3619974
Abstract

In the present study, the antitumor activity of some titanocene derivatives (C5H5)2TiX2 (I, X = Cl; II, X = Br; III, X = cis-OOCCH = CHCOOH; IV, X = p-SC6H4NH3+Cl-) was investigated against B16 melanoma and colon 38 carcinoma. Both tumors grew subcutaneously as solid tumors in mice. Substances were applied intraperitoneally either as single, triple or 5-fold injections. Against both tumors, satisfactory results were observed for the chloro, bromo and aminothiophenolato derivatives I, II and IV, resp. They reduced tumor growth by 60-80% to 40-20% of control values. These effects underline the antitumor potency of titanocene complexes and show that titanocene dihalides as well as titanocene derivatives containing hydrophilic ligands X are able to inhibit the growth of various solid experimental tumors.

摘要

在本研究中,研究了一些二茂钛衍生物(C5H5)2TiX2(I,X = Cl;II,X = Br;III,X =顺式 - OOCCH = CHCOOH;IV,X = p - SC6H4NH3 + Cl - )对B16黑色素瘤和结肠38癌的抗肿瘤活性。两种肿瘤均以实体瘤形式在小鼠皮下生长。物质通过单次、三次或5倍注射腹腔内给药。对于氯、溴和氨基硫酚盐衍生物I、II和IV,分别观察到对两种肿瘤均有令人满意的结果。它们将肿瘤生长降低至对照值的60 - 80%至40 - 20%。这些效应强调了二茂钛配合物的抗肿瘤效力,并表明二茂钛二卤化物以及含有亲水性配体X的二茂钛衍生物能够抑制各种实体实验肿瘤的生长。

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