Synthesis and biological activity of 5-aza-ellipticine derivatives.
Novel 5-aza-ellipticine derivatives were synthesized and tested as antitumor agents. The new compounds were prepared more readily than the analogous ellipticine derivatives, which are known to be potent anti-tumor agents Although the novel 5-aza-ellipticine derivatives are not as biologically active as their corresponding ellipticine analogues, the new compounds represent a new, readily accessible class of heteroaromatic catalytic inhibitors of topoisomerase II and possible anti-tumor agents.
Moody
Deborah L
DL
Structural Biophysics Laboratory, Molecular Aspects of Drug Design Section, Structural Biophysics Laboratory, NCI-Frederick, PO Box B Frederick, MD 21702, USA.
Dyba
Marcin
M
Kosakowska-Cholody
Teresa
T
Tarasova
Nadya I
NI
Michejda
Christopher J
CJ
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001372:Aza Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004611:Ellipticines / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
D000970:Antineoplastic Agents; D001372:Aza Compounds; D004611:Ellipticines; D059005:Topoisomerase II Inhibitors