86456-01-1

Upstream product

• 86455-99-4 2-<(3-chlorophenyl)thio>-5-methoxybenzoic acid 

Downstream Products

• 86456-05-5 1-<<2-(dimethylamino)ethyl>amino>-7-methoxy-9H-thioxanthen-9-one 

Relevant academic research and scientific papers

Thioxanthenone antitumor agents

Compounds having anti-tumour activity are disclosed having the formulawherein: (1) n is 2 or 3;R1 and R2 are independently lower-alkyl;Q is a residue chosen from the group consisting ofCH2NHR3, CH2N(R4)SO2R7, CH2NHCHO, CH=N-Ar,C(O)NR5R6, CH2N(R4)C(O)R7, CH2N(C2H5)CHO,CH2N(R4)P(O)(O-lower-alkyl)2, CH2N=CH-N(R9)(R10),CH2N(R4)C(O)CF3 and CH2N(R4)C(O)OR7;R3 is hydrogen or lower-alkyl;R4 is hydrogen, lower-alkyl or Ar;R5 is hydrogen, lower-alkyl or Ar;R6 is hydrogen or lower-alkyl;R7 is lower-alkyl, or Ar;R8 is hydroxy;Ar is phenyl or phenyl substituted with methyl, methoxy, hydroxy, halogen or nitro; andR9 and R10 are independently lower-alkyl; or(2) Q is a residue chosen from the group consisting of CH2N(R4)SO2R7, CH=N-Ar, C(O)NR5R6, CH2N(R4)C(O)R7, CH2N(R4)P(O)(O-lower-alkyl)2, CH2N(R4)C(O)CF3 and CH2N(R4)C(O)OR7; R8 is hydrogen, lower-alkyl, lower-alkoxy, or hydroxy; Ar is phenyl substituted by hydroxy; and n, R1, R2, R4, R5, R6, and R7 are as defined hereinabove in part (1) with the proviso that one or more of R4, R5, or R7 is Ar; or(3) Q is a residue chosen from the group consisting of CH2N=CH-N(R9)(R10) and CH2N(R4)C(O)CF3 ; R8 is hydrogen, lower-alkyl, lower-alkoxy, or hydroxy; and n, R1, R2, R4, R7, Ar, R9 and R10 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.

Analogues of hycanthone and lucanthone as antitumor agents

Hycanthone analogues (5 and 6) containing 7-substituted hydroxyl groups were prepared and evaluated as antitumor agents. These compounds were significantly more active than the corresponding unsubtituted derivatives. The 7-hydroxylated-4-(hydroxymethyl)-9H-xanthen-9-ones, 11 and 12, were also active antitumor agents. However, the 7-hydroxy-9H-xanthen-9-one counterparts of the 7-hydroxylucanthones were totally devoid of antitumor activity. Results obtained thus far are consistent with the hypothesis that 4-hydroxymethyl substituents in the 9H-xanthen-9-one and 9H-thioxanthen-9-one series are required for antitumor activity.