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Major groove binding and 'DNA-induced' fit in the intercalation of a derivative of the mixed topoisomerase I/II poison N-(2-(dimethylamino)ethyl)acridine-4-carboxamide (DACA) into DNA: X-ray structure complexed to d(CG(5-BrU)ACG)2 at 1.3-A resolution.

作者信息

Todd A K, Adams A, Thorpe J H, Denny W A, Wakelin L P, Cardin C J

机构信息

Chemistry Department, University of Reading, Whiteknights, Reading RG6 6AD, U.K.

出版信息

J Med Chem. 1999 Feb 25;42(4):536-40. doi: 10.1021/jm980479u.

DOI:10.1021/jm980479u
PMID:10052960
Abstract
摘要

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1
Major groove binding and 'DNA-induced' fit in the intercalation of a derivative of the mixed topoisomerase I/II poison N-(2-(dimethylamino)ethyl)acridine-4-carboxamide (DACA) into DNA: X-ray structure complexed to d(CG(5-BrU)ACG)2 at 1.3-A resolution.混合拓扑异构酶I/II抑制剂N-(2-(二甲基氨基)乙基)吖啶-4-甲酰胺（DACA）衍生物嵌入DNA时的大沟结合和“DNA诱导”契合：与d(CG(5-BrU)ACG)2形成的X射线晶体结构，分辨率为1.3埃
J Med Chem. 1999 Feb 25;42(4):536-40. doi: 10.1021/jm980479u.
2
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Extravascular transport of the DNA intercalator and topoisomerase poison N-[2-(Dimethylamino)ethyl]acridine-4-carboxamide (DACA): diffusion and metabolism in multicellular layers of tumor cells.DNA嵌入剂和拓扑异构酶毒物N-[2-(二甲基氨基)乙基]吖啶-4-甲酰胺（DACA）的血管外转运：在肿瘤细胞多层中的扩散与代谢
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J Med Chem. 1999 Jul 1;42(13):2383-93. doi: 10.1021/jm980687m.
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Structure-activity relationships for acridine-substituted analogues of the mixed topoisomerase I/II inhibitor N-[2-(dimethylamino)ethyl]acridine-4-carboxamide.混合拓扑异构酶I/II抑制剂N-[2-(二甲基氨基)乙基]吖啶-4-甲酰胺的吖啶取代类似物的构效关系
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