Methods for cancer therapy and stem cell modulation

A pharmaceutical composition, comprising

• (a) a compound of formula (I) or a pharmaceutically acceptable salt thereof,
• wherein in formula (I)
• A is C or N,
• R1, R4 and R5 are independently selected from the group consisting of H and aliphatic, cycloaliphatic, aromatic, arylaliphatic, and arylcycloaliphatic hydrocarbyl groups, comprising 0-3 heteroatoms selected from the group N, O, S, and Si,
• wherein R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge,
• R2 is selected from the group consisting of H and halogen, and
• R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms selected from the group N, O, S, Si, and halogen, and
• (b) a carrier or diluent.

A method of inducing apoptosis in a tumour cell, said method comprising administering to said tumour cell a compound of the general formula (I)

• wherein in formula (I)
• A is C or N,
• R1, R4 and R5 are independently selected from the group consisting of H and aliphatic, cycloaliphatic, aromatic, arylaliphatic, and arylcycloaliphatic hydrocarbyl groups, comprising 0-3 heteroatoms selected from the group N, O, S, and Si,
• wherein R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge,
• R2 is selected from the group consisting of H and halogen, and
• R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms selected from the group N, O, S, Si, and halogen.

A method for modulating gene expression in a cell that expresses the components of a polycomb repressive complex, said method comprising administering to said cell a compound of the general formula (I)

• wherein in formula (I)
• A is C or N,
• R1, R4 and R5 are independently selected from the group consisting of H and aliphatic, cycloaliphatic, aromatic, arylaliphatic, and arylcycloaliphatic hydrocarbyl groups, comprising 0-3 heteroatoms selected from the group N, O, S, and Si,
• wherein R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge,
• R2 is selected from the group consisting of H and halogen and
• R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms selected from the group N, O, S, Si, and halogen.