2-(1h-indol-3-yl)-2-oxo-acetamides with antitumor activity

Compounds of formula I

• 12
• wherein:
• R1, R2 and R5 are independently hydrogen or a C1-C6 alkyl group;
• R3 is hydrogen, C1-C4 alkyl, aralkyl, optionally substituted phenyl;
• R4 is hydrogen, straight or branched C1-C8 alkyl, C5-C6 cycloalkyl;
• aralkyl;
• heteroaralkyl;
• X is one or more groups, at most four, independently selected from hydrogen;
• C1-C6 alkyl;
• C1-C6 haloalkyl;
• C1-C6 hydroxyalkyl;
• C1-C6-aminoalkyl;
• C1-C6-alkoxy-C1-C6-alkyl;
• C1-C18-acyloxy-C1-C6-alkyl;
• hydroxy;
• C1-C4 alkoxy;
• C1-C3 haloalkoxy;
• phenoxy;
• aralkoxy;
• C1-C3 acyloxy;
• amino;
• C1-C3 alkylamino;
• C1-C3-acylamino;
• C1-C3-alkylsulfonylamino;
• aroylamino;
• halogen;
• nitro;
• cyano;
• trifluoromethyl;
• carboxy;
• C1-C6 alkoxycarbonyl;
• a RaRbN(CH2)nC(═O)— group wherein Ra and Rb are independently hydrogen, C1-C3-alkyl or Ra and Rb together with the nitrogen atom they are linked to form a pyrrolidino, piperidino, piperazino or morpholino ring and n=0 or an integer from 1 to 4;
• a RaRcN(CH2)nC(═O)— group wherein Ra and n are as above defined and Rc is a C1-C4-alkoxycarbonyl group;
• a R1C(═O)— group wherein R1 is as above defined;
• sulfonyl;
• mercapto;
• C1-C4-alkylthio;
• C1-C4-alkylsulfinyl;
• C1-C4-alkylsulfonyl;
• aminosulfonyl;
• C1-C3-alkylaminosulfonyl;
• a group —P(═O)(OR1)(OR2) being R1 and R2 as above defined;
• a group (E)- or (Z)-C(R1)═C(R2)—C(═O)R6 wherein R6 is hydroxy, C1-C6-alkoxy, NRaRb or a group of formula RaRbN(CH2)mNR1—, being m an integer from 2 to 4 and R1, R2, Ra, and Rb as above defined;
• Y is an oxygen or sulfur atom,
• the isomers, enantiomers and mixtures thereof,
• and the pharmaceutically acceptable salts thereof.