Antitumoral derivatives of ET-743

A compound of the general formula Ia:

• wherein R1 is C(═O)R′, C(═O)OR′, P═O(OR′)2, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, with the proviso that R1 is not acetyl;
• wherein R2, R4, R5 are each independently selected from H, C(═O)R′, C(═O)OR′, P═O(OR′)2, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl;
• wherein R6 and R7 are both ═O and the dotted lines indicate a quinone ring, or R6 is —OR3, where R3 is H, C(═O)R′, C(═O)OR′, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, R7 is H, and the dotted lines indicate a phenyl ring;
• wherein X2, X3, X4, X5, X6 are independently selected from H, OH, OR′, SH, SR′, SOR′, SO2R′, C(═O)R′, C(═O)OR′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, unsubstituted C1-C24 alkyl, unsubstituted C2-C18 alkenyl, unsubstituted C2-C18 alkynyl, unsubstituted C6-C18 carbocyclic aryl, and unsubstituted heteroaromatic selected from coumarinyl, quinolinyl, pyridyl, pyrazinyl, pyrimidyl, furyl, pyrrolyl, thienyl, thiazolyl, oxazolyl, imidazolyl, indolyl, benzofuranyl, benzothiazolyl tetrahyrdrofuranyl, tetrahydropyranyl, piperidinyl, morpholinyl and pyrolindinyl;
• wherein X1 is selected from hydrogen, hydroxy and cyano;
• wherein when R1, R2, R3, R4, and R5 are substituted, the substituents are each independently selected from the group consisting of OH, OR′, SH, SR′, SOR′, SO2R′, C(═O)R′, C(═O)OR′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, unsubstituted C1-C18 alkyl, unsubstituted C2-C18 alkenyl, unsubstituted C2-C18 alkynyl, unsubstituted C6-C18 carbocyclic aryl, and unsubstituted heterocyclic selected from coumarinyl, quinolinyl, pyridyl, pyrazinyl, pyrimidyl, furyl, pyrrolyl, thienyl, thiazolyl, oxazolyl, imidazolyl, indolyl, benzofuranyl, benzothiazolyl, tetrahydrofuranyl, tetrahydropyranyl, piperidinyl, morpholinyl and pyrolindinyl;
• wherein each of the R′ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, C(═O)H, C(═O)CH3, CO2H, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, and substituted or unsubstituted C6-C18 carbocylic aryl;
• and
• wherein when R′ is substituted, the substituents are each independently selected from the group consisting of halogen, cyano, hydroxyl, nitro, azido, unsubstituted C1-C6 alkanoyl, carboxamido, unsubstituted C1-C12 alkyl, unsubstituted C2-C12 alkenyl, unsubstituted C2-C12 alkynyl, unsubstituted C1-C12 alkoxy, unsubstituted C6-C18 carbocyclic aryloxy, unsubstituted C1-C12 alkylthio, unsubstituted C1-C12 alkylsulfinyl, unsubstituted C1-C12 alkylsulfonyl, unsubstituted C1-C12 aminoalkyl, unsubstituted C6-C18 carbocyclic aryl, unsubstituted aralkyl and unsubstituted heterocyclic group which is selected from coumarinyl, quinolinyl, pyridyl, pyrazinyl,pyrimidyl, furyl, pyrrolyl, thienyl, thiazolyl, oxazolyl, imidazolyl, indolyl, benzofuranyl, benzothiazolyl, tetrahydrofuranyl, tetrahydropyranyl, piperidinyl, morpholinyl and pyrolindinyl.