Indolocarbazole poisons of human topoisomerase I: regioisomeric analogues of ED-110.
Indolocarbazole poisons of human topoisomerase I: regioisomeric analogues of ED-110.
复制标题
人拓扑异构酶 I 的吲哚并咔唑毒物：ED-110 的区域异构类似物。
DOI：
10.1016/s0960-894x(98)00710-0
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发表时间：
1999
影响因子：
2.7
通讯作者：
Ames,MM
中科院分区：
文献类型：
--
作者：
Zembower,DE;Zhang,H;Lineswala,JP;Kuffel,MJ;Aytes,SA;Ames,MM
ED-110 是一种对人拓扑异构酶 I (Topo I) 具有有效活性的吲哚并咔唑衍生物，其所有四种“对称”区域异构体均已合成。与 ED-110 相比，在 3 位和 9 位含有羟基的异构体对 Topo I 的活性大约高出 10 倍，对人实体瘤细胞系的体外活性高出 5 至 35 倍。
All four “symmetrical” regioisomers of ED-110, an indolocarbazole derivative having potent activity against human topoisomerase I (Topo I) were synthesized. The isomer containing hydroxyl groups in the 3- and 9-positions was approximately ten-fold more active against Topo I, and 5- to 35-fold more active against human solid tumor cell lines in vitro, relative to ED-110.