Structure-activity relationship for DNA topoisomerase II-induced DNA cleavage by azatoxin analogues.
Structure-activity relationship for DNA topoisomerase II-induced DNA cleavage by azatoxin analogues.
复制标题
氮杂毒素类似物 DNA 拓扑异构酶 II 诱导 DNA 裂解的构效关系。
DOI：
10.1016/s0968-0896(97)00113-2
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发表时间：
1997
影响因子：
3.5
通讯作者：
Macdonald,TL
中科院分区：
文献类型：
--
作者：
Madalengoitia,JS;Tepe,JJ;Werbovetz,KA;Lehnert,EK;Macdonald,TL
Eighteen analogues of the nonintercalative DNA topoisomerase II (topo II)-active epipodophyllotoxin-ellipticine hybrid, azatoxin, were synthesized and evaluated for their ability to induce topo II-mediated DNA strand breaks in vitro. In general, the SAR profile of the azatoxins showed more homology with that of the epipodophyllotoxins than with the ellipticines. Of the compounds studied, only fluoro substitution at the 8-, 9, and 10-positions of azatoxins enhanced activity, with 9-fluoroazatoxin being the most active compound in this series.
