Design and synthesis of ellipticinium salts and 1,2-dihydroellipticines with high selectivities against human CNS cancers in vitro.

@article{Jurayj1994DesignAS,
  title={Design and synthesis of ellipticinium salts and 1,2-dihydroellipticines with high selectivities against human CNS cancers in vitro.},
  author={J Jurayj and Rudiger D. Haugwitz and Ravi K Varma and Kenneth D. Paull and John F. Barrett and Mark Cushman},
  journal={Journal of medicinal chemistry},
  year={1994},
  volume={37 14},
  pages={2190-7}
}
9-Methoxy-2-methylellipticinium acetate (6), along with the 9-methyl and 9-chloro derivatives (7, and 8, respectively) have shown remarkable selectivities in vitro against the NCI human CNS cancer subpanel. In order to target these types of compounds to the CNS in vivo, a series of 1,2-dihydroellipticines was synthesized. 9-Methoxy-2-methyl-1,2-dihydroellipticine (9) retained the potency and selectivity of the parent compound 6 but was unstable toward oxidation to 6. In order to improve the… CONTINUE READING