Selected derivatives of K-252a

A compound defined by the general formula (I):

• wherein:
• one R1 or R2 is selected from CO(CH2)jR4, CH(OH)(CH2)bR4A, (CH2)kR7, C≡C(CH2)nR13, HC═CH(CH2)mR12, HC═CH(CO2R33)2, CO(CH2)jSR27, CH2OR44, CH2CHR31CO2R32, and CHO;
• the other R1 or R2 is selected from hydrogen, lower alkyl, halogen, nitro, NR14R15, CH2SR37, CO(CH2)qR16, CH(OH)(CH2)eR38, (CH2)rR17, HC═CH(CH2)tR18, C≡C(CH2)uR19, CO(CH2)qSR37, CHO, CH(SR34)2, CH2CHR39CO2R40, and CH2OR36;
• R4 and R16 are selected from halogen, OR29, and NR5R6;
• R4A and R38 are selected from hydrogen, halogen and NR5R6;
• R5 and R6 are selected from hydrogen, lower alkyl, and phenyl;
• or R5 and R6 are combined with a nitrogen atom to form piperidine, morpholine, tetrahydropyrrole or piperazine;
• R7 and R17 are selected from halogen, phenyl, pyridyl, piperidinyl, morpholinyl, imidazolyl, OC(═O)H, OR9, NR10R11, CO2R8, N3, and SR27;
• R8 is selected from hydrogen, lower alkyl, phenyl, and pyridyl;
• R9 is selected from hydrogen, pyridylcarbonyl, and lower alkyl;
• R10 and R11 are selected from hydrogen, lower alkyl, hydroxyalkyl, phenyl, benzyl, methoxybenzyl, lower alkyloxycarbonyl, and lower alkylaminocarbonyl;
• or R10 and R11 combine together to form piperidine, morpholine, tetrahydropyrrole or piperazine;
• R12 and R18 are selected from hydrogen, lower alkyl, phenyl, pyridyl, imidazolyl, CO2R8, and NR10R11;
• R13 and R19 are selected from hydrogen, lower alkyl, NR10R11, and OR9;
• R14 and R15 are independently selected from hydrogen, lower alkyl, and lower alkylaminocarbonyl;
• R27 and R37 are selected from hydrogen, lower alkyl, hydroxyalkyl, phenyl, hydroxyphenyl, pyridyl, pyrimidine, thiazolinyl, benzothiazolyl, alkyltetrazole, benzimidazole, (CH2)2NMe2, and (CH2)aCO2R28;
• R28, R29, R32, R33, and R40 are selected from hydrogen and lower alkyl;
• R31 and R39 are selected from hydrogen and CO2R33;
• R34 is lower alkyl;
• R36 is selected from hydrogen, (CH2)2NMe2, methoxymethyl, ethoxymethyl, methoxyethyl, and ti-lower alkylsilyl in which the three lower alkyl groups are the same or different;
• R44 is selected from hydrogen, (CH2)2NMe2, methoxymethyl, ethoxymethyl, and methoxyethyl;
• a, b, and e are each 1 or 2;
• k and r are each 2, 3 or 4;
• m, n, t, and u are each 0 or 1;
• j and q are each 1, 2, 3, or 4;
• R3 is selected from hydrogen, acetyl, and lower alkyl;
• X is selected from hydrogen, hydroxymethyl, lower alkoxycarbonyl, and CONR20R21;
• R20 and R21 are independently selected from hydrogen and lower alkyl;
• Y is selected from hydroxy, lower alkoxy, aralkyloxy, and acyloxy;
• and
• each W1 and W2 is hydrogen or together represent oxygen.