Synthesis of dicationic diaryltriazines nucleic acid binding agents.

Synthesis of dicationic diaryltriazines nucleic acid binding agents.
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双二芳基三嗪核酸结合剂的合成。

DOI:
10.1016/0223-5234(94)90061-2
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发表时间:
1994
影响因子:
6.7
通讯作者:
Schinazi,Rf
Schinazi,Rf
中科院分区:
医学1区
文献类型:
--
作者:
Spychala,J;Boykin,Dw;Wilson,Wd;Zhao,M;Tidwell,Rr;Dykstra,Cc;Hall,Je;Jones,Sk;Schinazi,Rf

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The synthesis of 2,4-bis[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-1,3,5-triazine6aand 2,4-bis[4-(1,4,5,6-tetrahydropyrimidin-2-yl)phenyl]-1,3,5-triazine6bin 3 steps from either 4-bromobenzamidine or 4-(carbamoyl)benzamidine is reported. The synthesis of 4,6-bis[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-2-dimethylamino-1,3,5-triazine9aand 4,6-bis[4-(1,4,5,6-tetrahydropyrimidin-2-yl)phenyl]-2-dimethylamino-1,3,5-triazine9bin 2 steps from 1,4-dicyanobenzene is also described. The compounds6band9bbind strongly to DNA model sequences and inhibit topoisomerase II from 2 microbial sources. Compounds6aand9abind to both DNA and RNA model sequences whereas6band9bessentially do not bind to the RNA model.