77528-39-3Relevant articles and documents
Synthesis, DNA intercalation and antitumor activity of 9-hydroxy-11-demethylellipticine and some derivatives. Comparison with the corresponding ellipticines
Gouyette,Reynaud,Sadet,et al.
, p. 503 - 510 (2007/10/02)
The authors report 3 synthetic routes leading to the 11-demethylellipticines. Their 9-methoxylated and 9-hydroxylated derivatives as well as their quaternary ammonium salts have been compared with the corresponding ellipticine derivatives concerning their DNA affinity, their in vitro cytotoxic action and their in vivo antitumor activity. The experimental results indicate that the 11-demethylellipticines show less DNA affinity but possess a much lower toxicity than the corresponding ellipticines, being at the same time also less active on L 1210 leukemia. It appears that the presence of a methyl group on the intercalating ring (at C-11) plays a major role in determining the biological activity. A similar observation has been made in the actinomycin series.
