SYNTHESIS OF DICATIONIC DIARYLTRIAZINES NUCLEIC-ACID BINDING-AGENTS

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