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1-硝基-9-氨基吖啶衍生物的抗肿瘤活性

Antitumor activity of 1-nitro-9-aminoacridine derivatives.

作者信息

Hrabowska M, Mazerska Z, Lukowicz J P, Onoszko K, Ledóchowski A

出版信息

Arzneimittelforschung. 1982;32(9):1013-6.

PMID:6890816
Abstract

Results of studies on the antitumor activity of 26 newly synthetized 1-nitro-9-aminoacridine derivatives by means of in vitro and in vivo tests are presented. 15 derivatives among those showed repeated activity against the sarcoma growth. There were compounds with alkylaminopropyl chains, with hydroxyalkyl-aminoalkyl chains and also with hydroxyalkyl chains on amino group of 1-nitro-9-aminoacridine molecule. The other compounds with aminoacids in position 9 of 1-nitroacridine were active at higher doses. The remaining 7 compounds did not show any antitumor activity. Some aspects of the cellular antineoplastic response, as well as the morphologic appearance of the tumor invasion zone, were studied in comparison with the results of the screening tests. It seems that apart from the structural similarity each derivative has an individual influence on the host reactivity during the tumor growth.

摘要

本文展示了通过体外和体内试验对26种新合成的1-硝基-9-氨基吖啶衍生物的抗肿瘤活性研究结果。其中15种衍生物对肉瘤生长表现出反复的活性。这些化合物包括具有烷基氨基丙基链、羟烷基-氨基烷基链的,以及1-硝基-9-氨基吖啶分子氨基上带有羟烷基链的。其他在1-硝基吖啶9位带有氨基酸的化合物在较高剂量时有活性。其余7种化合物未表现出任何抗肿瘤活性。与筛选试验结果相比,研究了细胞抗肿瘤反应的一些方面以及肿瘤侵袭区域的形态外观。似乎除了结构相似性外,每种衍生物在肿瘤生长过程中对宿主反应性都有个体影响。

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