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所选三唑并及咪唑并吖啶酮类化合物的实验性抗肿瘤活性及毒性

Experimental antitumor activity and toxicity of the selected triazolo- and imidazoacridinones.

作者信息

Kuśnierczyk H, Chołody W M, Paradziej-Lukowicz J, Radzikowski C, Konopa J

机构信息

Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Wrocław.

出版信息

Arch Immunol Ther Exp (Warsz). 1994;42(5-6):415-23.

PMID:8572901
Abstract

Toxicity and antitumor effects of four compounds from the groups of triazoloacridinones and imidazoacridinones were evaluated in transplantable tumor systems in mice, including P388 leukemia, B16 melanoma and 2 colon adenocarcinomas C26 and C38. Tested compounds had moderate antileukemic activity but were active against B16 melanoma and 3 of them were very efficacious against colon tumors, providing high percentages of "cures". Toxicity for healthy mice, as well as antitumor activity, were found to depend on a treatment protocol. The compounds were better tolerated and gave higher antitumor effects when given as fractionated treatment. They displayed also sex-dependent toxicity and activity.

摘要

在小鼠可移植肿瘤系统中评估了三唑并吖啶酮类和咪唑并吖啶酮类的四种化合物的毒性和抗肿瘤作用,这些系统包括P388白血病、B16黑色素瘤以及两种结肠腺癌C26和C38。受试化合物具有中等抗白血病活性,但对B16黑色素瘤有活性,其中三种对结肠肿瘤非常有效,能提供高比例的“治愈”。发现对健康小鼠的毒性以及抗肿瘤活性取决于治疗方案。当采用分次给药治疗时,这些化合物耐受性更好且抗肿瘤效果更高。它们还表现出性别依赖性毒性和活性。

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