E2f activity inhibiting compound

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/47 (2006.01) A61K 38/08 (2006.01) A61K 38/17 (2006.01) C07K 7/08 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2267188

Compounds represented by the general formula (I): R1-A-R2 or pharmacologically acceptable salts thereof wherein R1 represents (un)substituted alkanoyl, (un)substituted aroyl, (un)substituted heteroarylcarbonyl, (un)substituted alkoxycarbonyl, (un)substituted aryloxycarbonyl, (un)substituted heteroaryloxycarbonyl, or hydrogen; R2 represents hydroxy, (un)substituted alkoxy or (un)substituted amino; and A represents a partial peptide sequence comprising at least 12 consecutive amino acid residues in the sequence of a dimer forming or DNA binding region of each member of E2F family.

Cette invention concerne des composés correpsondant à la formule générale (I): R?1¿-A-R?2¿ où R?1¿ représente un alcanoyle (non) substitué, un aroyle (non) substitué, un hétéroarylcarbonyle (non) substitué, un alcoxycarbonyle (non) substitué, un aryloxycarbonyle (non) substitué, un hétéroaryloxycarbonyle (non) substitué ou hydrogène. R?2¿ représente hydroxy, un alcoxy (non) substitué ou un amino (non) substitué. A représente enfin une séquence de peptide partielle, laquelle comprend au moins 12 résidus consécutifs d'acide aminé dans la séquence d'une région de formation d'un dimère ou de liaison d'ADN pour chaque membre de la famille E2F. Cette invention concerne également les sels de ces composés acceptables sur le plan pharmaceutique.

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