| 摘要 |
The present invention relates to novel compounds based on Troger base (TB) derivatives having two hydrazone groups (TB-bishydrazones), having substituted 2-hydroxyaryl group or heteroaryl group of the general formula I, in which Y represents H, CHi3, CHi2CHi3, with the proviso that Z=N or C-OH and X=A=C, than R1, R2, R3, R4 denote H, OH, alkyl containing 1 to 3 carbon atoms, allyl, a halogen, -CHi2OH, -OCHi3, -OCHi2CHi3, -CFi3, -CN, -COOCHi3, -COOCHi2CHi3, -NOi2, -SCHi3, -N(CHi3)i2, -N(CHi2CHi3)i2, -NHCHi3, -NHCOCHi3, R1, R2 or R2, R3 or R3, R4 represent CH=CH-CH=CH, i.e. a condensed benzene nucleus, with the proviso that Y denotes 2-pyridyl, than Z=N, X=A=C, R1, R2, R3, R4 are as specified above, with the proviso that Y represents H, CHi3, CHi2CHi3, and Z=N, X=N and A=C, than R1 and R2 are as specified above and R3 is not present and R4 denotes H, OH, alkyl having 1 to 3 carbon atoms, allyl, a halogen, -CHi2OH, -OCHi3, -OCHi2CHi3, -CFi3, -CN, -COOCHi3, -COOCHi2CHi3, -NOi2, -SCHi3, -N(CHi3)i2, -N(CHi2CHi3)i2, -NHCHi3, -NHCOCHi3 with the proviso that Y=H, Z=C-OH, A=N and X=C, than R1=CHi3, R2 is not present, Ri3=H and R4=CHi2OH. These compounds exhibit cytostatic activity and can be therefore used in the preparation of therapeutics for the treatment of tumor diseases. |
