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Synthesis of dicationic diaryltriazines nucleic acid binding agents.

Abstract：

:- The synthesis of 2,4-bis[4-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-1,3,5-triazine 6a and 2,4-bis[4-(1,4,5,6-tetrahydropyrimidin-2-yl)phenyl]-1,3,5-triazine 6b in 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-triazine 9a and 4,6-bis[4-(1,4,5,6-tetrahydropyrimidin-2-yl)phenyl]-2-dimethylamino-1,3,5-triazine 9b in 2 steps from 1,4-dicyanobenzene is also described. The compounds 6b and 9b bind strongly to DNA model sequences and inhibit topoisomerase II from 2 microbial sources. Compounds 6a and 9a bind to both DNA and RNA model sequences whereas 6b and 9b essentially do not bind to the RNA model.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Spychala J,Boykin D,Wilson W,Zhao M,Tidwell R,Dykstra C,Hall J,Jones S,Schinazi R

doi

10.1016/0223-5234(94)90061-2

subject

Has Abstract

pub_date

1994-01-01 00:00:00

pages

363-367

issue

5

eissn

0223-5234

issn

1768-3254

pii

0223-5234(96)88214-6

journal_volume

29

pub_type

杂志文章

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