1,4-Dimethoxy-9(10H)-acridinone derivatives. Synthesis, DNA binding studies and trypanocidal activity.
New acridinonic derivatives, which are hydroxy- and methoxy-substituted in positions 1, 4, and 1,4 were prepared with a view to obtain antiparasitic drugs. These compounds were tested against Trypanosoma cruzi strains and their capability of interacalation into DNA was determined. Nucleus substitutions, DNA binding, and trypanocidal activities have been correlated.
Berny
H
H
Groupe d'Enseignement et de Recherce en Chimie, Thérapeutique Organique et Physique (GERCTOP), Faculté de Pharmacie, Université de Marseille, France.
Bsiri
N
N
Charbit
J J
JJ
Galy
A M
AM
Soyfer
J C
JC
Galy
J P
JP
Barbe
J
J
Sharples
D
D
Mesa Valle
C M
CM
Mascaro
C
C
D000166:Acridines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002467:Cell Nucleus / Q000187:drug effects / Q000378:metabolism; D004247:DNA; D016054:DNA, Protozoan / Q000187:drug effects* / Q000378:metabolism; D007364:Intercalating Agents / Q000494:pharmacology; D051379:Mice; D008807:Mice, Inbred BALB C; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000378:metabolism; D014349:Trypanosoma cruzi / Q000187:drug effects
D000166:Acridines; D016054:DNA, Protozoan; D007364:Intercalating Agents; D014344:Trypanocidal Agents; D004247:DNA