The present invention is directed, in general, to methods for treating human cancers and in particular to new compounds which cross the blood brain barrier and retain activity against CNS specific cancer cell lines, to pharmaceutical formulations containing such compounds, and to methods for the treatment of cancer.

The 2-methylellipticinium salts offer remarkable examples of compounds that have shown selective cytotoxicity for the CNS cancer cell lines. In 17 assays, 6 showed selectivity for the CNS subpanel at every level of the dose-response curve down to 10-7M. Both the 9-methyl and the 9-chloro analogues also displayed good CNS selectivity at the levels for growth inhibition and cytostasis.

This research is described, in part, in Jurayj et al., "Design and Synthesis of Ellipticinium Salts and 1,2- Dihydroellipticines with High Selectivities against Human CNS Cancers in vitro," J. Med. Chem. 37(14):2190-2197, 1994.

U.S. Patent No. 5,272,146 issued 21 Dec 1993 (HHS Reference No. E-110-1992/0-US-01); U.S. Patent No. 5,441,941 issued 15 Aug 1995 (HHS Reference No. E-110- 1992/0-US-02)

Inventors: Rudiger D. Haugwitz (NCI) et al.

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