Inhibitors of the e2f-1/cyclin interaction for cancer therapy

C - Chemistry – Metallurgy – 07 – K

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C07K 7/06 (2006.01) A61K 38/08 (2006.01) A61P 35/00 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2432031

The novel compounds of this invention have the general structural formula la- d: The compounds of this invention relate to 8-mer, 7-mer, 6-mer and 5-mer peptides having the following amino acid sequences, and referred to collectively as having "formula la-d": or a pharmaceutically acceptable salt or ester thereof, that inhibit the interaction of the transcription factor E2F- 1 to Cyclin A. As an antagonist of the E2F-1/Cyclin A interaction, the compounds of the present invention may be used in the treatment of cancer.

La présente invention concerne de nouveaux composés représentés par la formule développée la-d. Les composés selon l'invention concernent les peptides 8-mer, 7-mer, 6-mer et 5-mer comprenant les séquences d'acides aminés suivantes et auxquels on se réfère sous l'appellation collective de composés 'de formule Ia-d''. Ces composés ou un sel ou un ester pharmaceutiquement acceptable de ces derniers inhibent l'interaction du facteur de transcription E2F-1 et de la Cycline A. On peut utiliser, dans le traitement des cancers, les composés de la présente invention, en tant qu'antagonistes de l'interaction E2F-1/Cycline. Formule Ia-d

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