Synthesis and biological properties of new benz[h]isoquinoline derivatives.
In order to determine the importance of the pyrrolic nitrogen atom in a series of suitably substituted gamma-carbolines derivatives for their cytotoxic and antitumor properties, a series of structurally related benz[h]isoquinolines were synthesized. When compared to the "parent" gamma-carbolines, these new compounds showed greatly decreased effects on topoisomerases I and II. Whereas the 8-hydroxylated derivatives retained a significant cytotoxicity, all the new compounds were devoid of antitumor effect in the P388 murine ip-ip system.
URA 1387 CNRS, Institut Curie Section de Biologie, Centre Universitaire, Orsay, France.
Y L
YL
Janin
D
D
Carrez
J F
JF
Riou
E
E
Bisagni
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D005260:Female; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000633:toxicity; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains
D000970:Antineoplastic Agents; D007546:Isoquinolines