Synthesis of Dicationic Diaryltriazines Nucleic Acid Binding Agents

Jaroslaw Spychala

doi:https://doi.org/10.1016/0223-5234(94)90061-2

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 and 2,4-bis[4-(1,4,5,6-tetrahydropyrimidin-2-yl)phenyl]-1,3,5-triazine I (R = H, n = 2, 3) 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 and 4,6-bis[4-(1,4,5,6-tetrahydropyrimidin-2-yl)phenyl]-2-dimethylamino-1,3,5-triazine I (R = NMe2, n = 2, 3) in 2 steps from 1,4-dicyanobenzene is also described. The compds. I (R = H, NMe2, n = 3) bind strongly to DNA model sequences and inhibit topoisomerase II from 2 microbial sources. Compds. I (R = H, NMe2, n = 2) bind to both DNA and RNA model sequences whereas I (R = H, NMe2, n = 3) essentially do not bind to the RNA model.

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Jaroslaw Spychala dr

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Category:: Magazine publication
Type:: Magazine publication
Published in:: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY no. 29, edition 5, pages 363 - 367,
ISSN: 0223-5234
Publication year:: 1994
Bibliographic description:: J Spychala, DW Boykin, WD Wilson, M Zhao, RR Tidwell, CC Dykstra, JE Hall, SK Jones, RF Schinazi, Synthesis of Dicationic Diaryltriazines Nucleic Acid Binding Agents. European Journal of Medicinal Chemistry, vol. 29(5), pages 363-367, 1994.
DOI:: Digital Object Identifier (open in new tab) https://doi.org/10.1016/0223-5234(94)90061-2
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