| 摘要 |
<p>A quinone imine enediyne possessing cytotoxic activity towards cancer cells having general structure (I) wherein R1, R2 and R3 are independently the same or different and are H, Br, Cl, F, NH2, CO2H, OH, linear or branched alkyl, etc.; wherein R4 is H, OH or linear or branched alkoxy, linear or branched alkoxycarbonyl, etc.; wherein R5 is H, Br, Cl, F, O=, OH or S-SR, or linear or branched alkyl, etc.; wherein R6 is H, Br, Cl, F, CO2H, OH or S-SR', or linear or branched alkyl, etc.; wherein R7 is H, OH or S-SR', or linear or branched alkyl, linear or branched alkoxycarbonyl, linear or branched alkoxy or linear or branched hydroxyalkyl; and wherein R, R' and R' are independently the same or different and are linear or branched alkyl, linear or branched acyl or linear or branched alkoxyalkyl. Also provided are conjugates of the compound with cleavable peptides, enzymes, carbohydrates and monoclonal antibodies immunoreactive with cancer cells, as well as compositions comprising the analogues and conjugates, and methods of synthesis and treatment of tumors.</p> |
