abstract |
The present invention provides illudin analogs of the general formula (I): n n n n n n n n n n n n where R 1 is (CH 2 ) 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 (C 1 -C 8 )alkyl, (C 6 -C 10 )aryl, (C 6 -C 10 )aryl(C 1 -C 4 )alkyl or cyclo(C 3 -C 6 )alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; n R 2 is absent; or R 1 and R 2 together comprise a 5-7 membered cyclic ring; n R 3 is (C 1 -C 4 )alkyl or H; R 4 is H, SCH 2 CO 2 (C 1 -C 4 )alkyl, O—(C 5 -C 12 )aryl or —S—(C 5 -C 12 )aryl; R 5 is H, OH or absent; R 6 is (C 1 -C 4 )alkyl or absent; R 7 is OH or OSi((C 1 -C 4 )alkyl) 3 ; or n R 6 and R 7 together are ethylenedioxy; n R 8 is optionally substituted (C 1 -C 4 )alkyl; and n the bonds represented by ----- are individually present or absent. The invention further provides dimers comprising analogs of formula (I). |