Polycyclic aromatic compounds as anticancer agents: Structure-activity relationships of chrysene and pyrene derivatives
Polycyclic aromatic compounds as anticancer agents: Structure-activity relationships of chrysene and pyrene derivatives
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DOI：
10.1016/s0968-0896(00)00297-2
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发表时间：
2001-03-01
影响因子：
3.5
通讯作者：
Becker, FF
中科院分区：
文献类型：
--
作者：
Banik, BK;Becker, FF
以6-氨基芘和1-氨基芘为原料，合成了大量的二酰胺和二胺。以顺铂为内对照，对动物和人肿瘤细胞系进行了体外构效关系研究。该研究表明，对这些细胞系的体外细胞毒性取决于分子中存在的功能。二氨基化合物被发现是更有效的比二酰胺，这些都是同样的活性，无论末端杂环基团，而活性的二酰胺是强烈依赖于终端单元。一般来说，含芘的二酰胺比含芘的二酰胺的活性高。末端杂环的大小，沿着连接多环与杂环的间隔基的性质，似乎影响某些细胞系中的生物活性。对先导化合物进行的溶血实验表明，其活性与膜稳定剂的活性相似。该试剂还证明了在白血病细胞系中产生分化的能力。(C)2001爱思唯尔科技有限公司版权所有。
A large number of diamides and diamines were synthesized using 6-amino chrysene and 1-amino pyrene as starting materials. A structure-activity study with cis-platinum as internal control against animal and human tumor lines was carried out in vitro. This study indicated that the in vitro cytotoxicity toward these lines depends on the functionality present in the molecules. The diamino compounds were found to be more potent than the diamides, and these were equally active irrespective of the end heterocyclic group, whereas the activity of the diamides was strongly dependent on the terminal unit. In general, the diamides containing chrysene as the chromophore were more active than those with a pyrene ring. The size of the end heterocyclic ring, along with the nature of the spacer connecting the polycyclic ring to the heterocyclic ring, seemed to affect the biological activity in certain cell lines. Hemolysis experiments on a lead compound established that it had activities similar to those described for membrane-stabilizing agents. This agent also demonstrated the capacity to produce differentiation in leukemia cell lines. (C) 2001 Elsevier Science Ltd. All rights reserved.