Antitumoral analogs of et-736

C - Chemistry – Metallurgy – 07 – D

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C07D 515/22 (2006.01) A61K 31/438 (2006.01) A61K 31/4985 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2455768

Derivatives of ecteinascidin 736 of general formula (I) wherein the groups R1, R2, R3, R4 and R5 are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO2R', C(=O)R', C(=O)OR', NO2, NH2, NHR', N(R')2, NHC(O)R', CN, halogen, =O, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2- C18 alkynyl, substituted or unsubstituted arly, substituted or unsubstituted heterocyclic; wherein X is independently selected of OR', CN, (=O), or H; wherein each of the R' groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, =O, C(=O)H, C(=O)CH3, CO2H, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein m is 0, 1 or 2; and wherein n is 0, 1, 2, 3, or 4, and their use as antitumoral agent.

Dévirés d'ectéinascidine 736 représentés par la formule générale (I) dans laquelle les groupes R¿1?, R¿2?, R¿3?, R¿4? et R¿5? sont sélectionnés indépendamment chacun dans le groupe constitué par H, OH, OR', SH, SR', SOR', SO¿2?R', C(=O)R', C(O)R', NO¿2?, NH¿2?, NHR', N(R'), NHC(O)R'. CN, halogène, =O, alkyle C¿1?-C¿25? substitué ou non substitué, alkényle C¿2?-C¿18? substitué ou non substitué, alkynyle C¿2?-C¿18? substitué ou non substitué, aryle substitué ou non substitué, un composé hétérocyclique substitué ou non substitué; X est sélectionné indépendamment dans OR', CN, (=O), ou H. Chacun des groupes R' est sélectionné indépendamment dans un groupe constitué par H, OH, NO¿2?, NH¿2?, SH, CH, halogène, =O, C(=O)H, C(=O)CH¿3?, CO¿2?H, alkyle C¿1?-C¿25? substitué ou non substitué, alkényle C¿2?-C¿18? substitué ou non substitué, alkynyle C¿2?-C¿18? substitué ou non substitué, aryle substitué ou non substitué; m est 0, 1 ou 2 et n est 0, 1, 2, 3 ou 4, ainsi que leur utilisation en tant qu'agent antitumoral.

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