Synthesis and biological evaluation of dialkylaminoalkylamino benzo[c][1,7] and [1,8]phenanthrolines as antiproliferative agents.
Benzo[c][1,7] and [1,8]phenanthroline substituted by dialkylaminoalkyl side chains at position C2 and C1, respectively, were synthesized and their biological activity evaluated. These compounds displayed more potent cytotoxicity toward L1210 cells than the parent unsubstituted compounds, associated with strong DNA interaction. The moderate TopoI inhibitory activity induced by the novel compounds suggests that other cellular targets should be responsible for the antiproliferative activity.
Laboratoire de Pharmacognosie de l'Université Paris Descartes, U.M.R./C.N.R.S. n degrees 8638, Faculté de Pharmacie, 4 Avenue de l'Observatoire, 75006 Paris, France.
Tuba
T
Serbetçi
Constance
C
Genès
Sabine
S
Depauw
Soizic
S
Prado
François-Hugues
FH
Porée
Marie-Paule
MP
Hildebrand
Marie-Hélène
MH
David-Cordonnier
Sylvie
S
Michel
François
F
Tillequin
D000818:Animals; D001483:Base Sequence; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002942:Circular Dichroism; D004247:DNA / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D006801:Humans; D051379:Mice; D008969:Molecular Sequence Data; D009691:Nucleic Acid Denaturation; D010618:Phenanthrolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D013056:Spectrophotometry, Ultraviolet; D013379:Substrate Specificity; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors
D010618:Phenanthrolines; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D004247:DNA