The University of British Columbia

Cornell Research Foundation Inc.

University of Alberta

E Dilip De Silva

Raymond John Andersen

Theresa M Allen

Jon C Clardy

Michel Roberge

Robert A Britton

Julie S Racok

Linda S Brinen

This invention provides analogs of eleutherobin and the eleuthesides modified at the C-11 position or comprising an epoxide functionality from C-11 to C-12. C-11 to C-12 is an ideal location for conjugating functional moieties to the eleutherobin pharmacophore without significant loss of antimitotic activity. Moieties that may be conjugated at C-11 include those intended to increase the solubility of the pharmacophore, to facilitate drug formulation, or to facilitate in vivo delivery or targeting.

Antimitotic eleuthesides

5-Methylimidazo[4,5-e]-1,2-thiazin-4(5-H)-one, having the structure ##STR1## a cytotoxic metabolite of the marine sponge Neamphius huxleyi, has been isolated from the sponge by extraction and chromatography.

Biologically active thiazine

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Vancouver, Canada

E Dilip De Silva