| 摘要 |
<p>Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of general structure (I), wherein E is H, CO2R, CONH2, CONHR, CONR2, acyl, or CN; X is H, OH, or OR; R?1, R2, R3 and R4¿ are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R?5, R6, R7, R8 and R9¿ are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, alkoxy, hydroxyalkyl, or aminoalkoxy group, or an aryl or aryloxy group, or a C-glycal, or CO¿2?R, nitro, cyano, Cl, F, Br, I, SR?10, NR11R12, or OR13¿; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R?10, R11 and R12¿ are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, hydroxyalkyl, or acyl group, or an aryl group; R13 is glycosyl; n is 0 or 1; with the proviso that when R1 is ethyl, and n is 0, E, R?2, R3 and R4¿ are not all H. Intermediate compounds leading to the camptothecin analogues comprise substituted tricyclic compounds which consist of rings C, D and E fused together. Methods for preparing the analogues involve condensation of such intermediates with variably substituted protected α-aminobenzaldehydes.</p> |
