| abstract |
The invention relates to epothilone analog represented by formula (I) wherein (i) R2 is absent or oxygen; 'a' can be either a single or double bond; 'b' can be either absent or a single bond; and 'c' can be either absent or a single bond, with the proviso that if R2 is oxygen then 'b' and 'c' are both a single bond and 'a' is a single bond; if R2 is absent then 'b' and 'c' are absent and 'a' is a double bond; and if 'a' is a double bond, then R2, 'b' and 'c' are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; -CH=CH2; -C CH; -CH2F; -CH2Cl; -CH2-OH; -CH2-O-(C1-C6-alkyl); and -CH2-S-(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of formula (I) where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerisation inhibiting activity and are e.g. useful against proliferative diseases. |