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Abstract

The invention provides variolin derivatives of formula (I), wherein: R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, OH, OR, SH, SR, SOR, SO.sub.2R, NO.sub.2, NH.sub.2, NHR, N(R).sub.2, NHCOR, N(COR).sub.2, NHSO.sub.2R, CN, halogen, C(.dbd.O)H, C(.dbd.O)R, CO.sub.2H, CO.sub.2R, C.sub.1-C.sub.12 alkyl, C.sub.1-C.sub.12 haloalkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; and R.sub.3 is selected from the group consisting of H, OH and OMe; wherein the or each group R is independently selected from the group consisting of OH, C.sub.1-C.sub.12 alkyl, C.sub.1-C.sub.12 haloalkyl, C.sub.2-C.sub.12 alkenyl, C.sub.2-C.sub.12 alkynyl, substituted or unsubstituted aryl, substituted unsubstituted aralkyl, substituted or unsubstituted arylalkenyl and substituted or unsubstituted heteroaromatic, and wherein the group R.sub.1, R.sub.2 or R.sub.3 is a group of formula N(R).sub.2 or N(COR).sub.2, each of the R groups may be the same or different, or the two R groups, together with the nitrogen atom to which they are attached, may form a 5-14 membered heterocyclic ring. These compounds display activity against a range of mammalian cancer cell lines. New synthetic routes to new and known variolin compounds, together with novel intermediates, are also disclosed. New antitumour activity of known variolin compounds is also described.

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First Claim