Thioxanthenone antitumor agents

摘要

Compounds having anti-tumour activity are disclosed having the formula wherein: (1) n is 2 or 3; R<1> and R<2> are independently lower-alkyl; Q is a residue chosen from the group consisting of CH2NHR<3>, CH2N(R<4>)SO2R<7>, CR2NHCHO, CH=N-Ar, C(O)NR<5>R<6>, CH2N(R<4>)C(O)R<7>, CH2N(C2H5)CHO, CH2N(R<4>)P(O)(O-lower-alkyl)2, CH2N=CH-N(R<9>)(R<10>), CH2N(R<4>)C(O)CF3 and CH2N(R<4>)C(O)OR<7>; R<3> is hydrogen or lower-alkyl; R<4> is hydrogen, lower-alkyl or Ar; R<5> is hydrogen, lower-alkyl or Ar; R<6> is hydrogen or lower-alkyl; R<7> is lower-alkyl, or Ar; R<8> is hydroxy; Ar is phenyl or phenyl substituted with methyl, methoxy, hydroxy, halogen or nitro; and R<9> and R<10> are independently lower-alkyl; or (2) Q is a residue chosen from the group consisting of CH2N(R<4>)SO2R<7>, CH=N-Ar, C(O)NR<5>R<6>, CH2N(R<4>)C(O)R<7>, CH2N(R<4>)P(O)(O-lower-alkyl)2, CH2N(R<4>)C(O)CF3 and CH2N(R<4>)C(O)OR<7>; R<8> is hydrogen, lower-alkyl, lower-alkoxy, or hydroxy; Ar is phenyl substituted by hydroxy; and n, R<1>, R<2>, R<4>, R<5>, R<6>, and R<7> are as defined hereinabove in part (1) with the proviso that one or more of R<4>, R<5>, or R<7> is Ar; or (3) Q is a residue chosen from the group consisting of CH2N=CH-N(R<9>)(R<10>)and CH2N(R<4>)C(O)CF3 ; R<8> is hydrogen, lower-alkyl, lower-alkoxy, or hydroxy; and n, R<1>, R<2>, R<4>, R<7>, Ar, R<9> and R<10> are as defined hereinabove in part (1), or a pharmaceutically acceptable acid-addition salt or solvate thereof . Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.