1-氨基取代的4-甲基-5H-吡啶并[3',4':4,5]吡咯并[3,2-c]吡啶：一类新型抗肿瘤药物。
1-Amino-substituted 4-methyl-5H-pyrido[3',4':4,5]pyrrolo[3,2-c]pyridines: a new class of antineoplastic agents.
作者信息
Nguyen C H, Bisagni E, Pepin O, Pierré A, de Cointet P
出版信息
J Med Chem. 1987 Sep;30(9):1642-7. doi: 10.1021/jm00392a021.
In an attempt to find new anticancer agents, a series of pyrido[3',4':4,5]pyrrolo[3,2-c]pyridines were synthesized and evaluated in the standard NCI screening. Among these new compounds, which are structurally related to 9-azaellipticines but differ by deletion of a cycle, those that have a 4-methyl group and a NHCH2CH2CH2NR2 side chain at the 1-position show significant cytotoxicity on L1210 cultured cells and antitumor properties in the in vivo P388 leukemia system. The in vivo antineoplastic activity of the most potent compounds were confirmed on the L1210 leukemia model.
为了寻找新的抗癌药物，合成了一系列吡啶并[3',4':4,5]吡咯并[3,2-c]吡啶，并在标准的美国国立癌症研究所（NCI）筛选中进行了评估。在这些与9-氮杂椭圆玫瑰树碱结构相关但因缺失一个环而不同的新化合物中，那些在1位具有4-甲基和NHCH2CH2CH2NR2侧链的化合物对L1210培养细胞显示出显著的细胞毒性，并在体内P388白血病系统中具有抗肿瘤特性。在L1210白血病模型上证实了最有效化合物的体内抗肿瘤活性。
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