Variolin derivatives and their use as antitumor agents

Details Variolin derivatives and their use as antitumor agents Variolin derivatives and their use as antitumor agents

C - Chemistry, Metallurgy

07

D

C07D 471/14 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) C07D 401/06 (2006.01)

Patent

CA 2453418

Variolin derivatives of formula (5) are provided: (see formula 5) wherein the substituent groups defined by X2, R1, R2, R3, R6, R7 and R12 are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO2R', NO2, NH2, NHR', N(R')2, NHCOR', NHSO2R', CN, halogen, =O, C(=O)H, C(=O)R', CO2H, CO2R', carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R' groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, =O, C(=O)H, C(=O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.

Cette invention concerne des dérivés de varioline représentés par la formule (5), selon laquelle les groupes substituants définis par X¿2?, R¿1?, R¿2?, R¿3?, R¿6?, R¿7? et R¿12? sont chacun indépendamment sélectionnés dans le groupe comprenant H, OH, OR', SH, SR', SOR', SO¿2?R', NO¿2?, NH¿2?, NHR', N(R')¿2?, NHCOR', NHSO¿2?R', CN, halogène, =O, C(=O)H, C(=O)R', CO¿2?H, CO¿2?R', carboxyalkyl, alkyle C¿1?-C¿12?, alcényle C¿2?-C¿12?, alcynyle C¿2?-C¿12?, aryle substitué ou non substitué, aralkyle substitué ou non substitué et hétéroaromatique substitué ou non substitué ; chacun des groupes R' est indépendamment sélectionné dans le groupe contenant H, OH, SH, N0¿2?, NH¿2?, CN, halogène, =O, C(=O)H, C(=O)CH¿3?, CO¿2?H, CO¿2?CH¿3?, alkyle C¿1?-C¿12?, alcényle C¿2?-C¿12?, alcynyle C¿2?-C¿12?, aryle, aralkyle et hétéroaromatique ; et les paires de groupes R¿1? et R¿2?, R¿2? et R¿3?, R¿3? et R¿12?, R¿12? et R¿6?, ou R¿6? et R¿7? peuvent être reliées en un système de noyau carbocyclique ou hétérocyclique.

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