8-取代的5-[(氨基烷基)氨基]-6H-γ-三唑并[4,5,1-de]吖啶-6-酮作为潜在的抗肿瘤药物。合成与生物活性。
8-Substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones as potential antineoplastic agents. Synthesis and biological activity.
作者信息
Cholody W M, Martelli S, Konopa J
机构信息
Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdansk, Poland.
出版信息
J Med Chem. 1990 Oct;33(10):2852-6. doi: 10.1021/jm00172a028.
PMID:2213837
Abstract
A series of 8-substituted 5-[(aminoalkyl)amino]-6H-v-triazolo[4,5,1-de]acridin-6-ones (2), structurally related to the imidazoacridinones (1), was synthesized and tested for cytotoxic and antineoplastic activity. Preliminary biological results indicated that the 8-OH derivatives possess the highest antitumor activity. No relationship has been found between the nature of the C-8 substituent and antitumor activity.
摘要
合成了一系列与咪唑并吖啶酮（1）结构相关的8-取代-5-[(氨基烷基)氨基]-6H-γ-三唑并[4,5,1-de]吖啶-6-酮（2），并对其细胞毒性和抗肿瘤活性进行了测试。初步生物学结果表明，8-羟基衍生物具有最高的抗肿瘤活性。未发现C-8取代基的性质与抗肿瘤活性之间存在关联。
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