Illudin analogs useful as antitumor agents

摘要

The present invention provides illudin analogs of the general formula (I): where R₁ is (CH₂)_n-X-Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C₁-C₈)alkyl, (C₆-C₁₀)aryl, (C₆-C₁₀)aryl(C₁-C₄)alkyl or cyclo(C₃-C₆)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R₂ is absent; or R₁ and R₂ together comprise a 5-7 membered cyclic ring; R₃ is (C₁-C₄)alkyl or H; R₄ is H, SCH₂CO₂(C₁-C₄)alkyl, O-(C₅-C₁₂)aryl or -S-(C₅-C₁₂)aryl; R₅ is H, OH or absent; R₆ is (C₁-C₄)alkyl or absent; R₇ is OH or OSi((C₁-C₄)alkyl)₃; or R₆ and R₇ together are ethylenedioxy; R₈ is optionally substituted (C₁-C₄)alkyl; and the bonds represented by --- are individually present or absent. The invention further provides dimers comprising analogs of formula (I).