Pyrene-linked pyrrolo (2,1-c) (1,4) benzodiazepine...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/5517 (2006.01) A61P 35/00 (2006.01) C07D 209/00 (2006.01) C07D 243/00 (2006.01)

Patent

CA 2520901

The present invention relates to pyrrolo [2,1-c][1,4]benzodiazepine hybrids useful as potential antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. More particularly, it provides 7-methoxy-8-[N- (1~-pyrenyl)-alkane-3.prime.-carboxamide]-oxy-(11aS)-1,2,3,11a-tetraydro 5H- pyrrolo[2,1-c][1,4]benzodiazepin-5-one, with aliphatic chain length variation of these compounds and it also describes the DNA binding, anticancer (antitumour) activity. The structural formula of this novel pyrrolo[2,1- c][1,4]benzodiazepine is given below, formula (I):

La présente invention a trait à des hybrides pyrrolo [2,1-c][1,4]benzodiazépine utiles en tant qu'agents antitumoraux potentiels. L'invention a également trait à un procédé pour la préparation de nouveaux hybrides pyrrolo [2,1-c][1,4]benzodiazépine en tant qu'agents antitumoraux potentiels. Plus particulièrement, l'invention a trait à de nouveaux composés de 7-méthoxy-8-[N-(1''-pyrényl)-alcane-3'-carboxamide]-oxy-(11a<I>S</I>)-1,2,3,11a-tétrahydro 5<I>H</I>-pyrrolo[2,1-<c][1,4]benzodiazépin-5-one, avec variation de longueur de chaîne aliphatique de ces composés ainsi qu'à l'activité anticancéreuse (antitumorale) de liaison à l'ADN. Les nouveaux composés de l'invention sont de formule générale (I).

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