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1. 发明申请

WO1994011376A1 CAMPTOTHECIN ANALOGUES AND METHODS OF PREPARATION THEREOF 审中-公开
标题翻译： CAMPTOTHECIN类似物及其制备方法
公开(公告)号：WO1994011376A1
公开(公告)日：1994-05-26
申请号：PCT/US1993006918
申请日：1993-07-23
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , DANISHEFSKY, Samuel, J. , BORNMANN, William, G. , SHEN, Wang , COBURN, Craig, A.
IPC分类号： C07D491/14
CPC分类号： C07D491/14 , C07H17/00
摘要： 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 , R , R and R 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 , R , R , R and R 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 CO2R, nitro, cyano, Cl, F, Br, I, SR , NR R , or OR ; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R , R and R 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; R is glycosyl; n is 0 or 1; with the proviso that when R is ethyl, and n is 0, E, R , R and R 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 alpha -aminobenzaldehydes.
摘要翻译：具有一般结构（I）的癌细胞具有细胞毒性活性的喜树碱的取代类似物，其中E是H，CO 2 R，CONH 2，CONHR，CONR 2，酰基或CN; X是H，OH或OR; R 1，R 2，R 3和R 4独立地相同或不同，为H，或直链或支链烷基，烷基芳基或羟基烷基或芳基; R 5，R 6，R 7，R 8和R 9独立地相同或不同，为H，或直链或支链烷基，烷基芳基，烷氧基，羟基烷基或氨基烷氧基氰基，Cl，F，Br，I，SR 10，NR 11 R 12或OR 13中的至少一个或多个。 R是H或直链或支链烷基，烷基芳基或羟基烷基或芳基; R 10，R 11和R 12独立地相同或不同，为H，或直链或支链烷基，烷芳基，羟基烷基或酰基或芳基; R 13是糖基; n为0或1; 条件是当R 1是乙基且n是0时，E，R 2，R 3和R 4不是全部H.导致喜树碱类似物的中间体化合物包括取代的三环化合物，其中由融合在一起的环C，D和E组成。制备类似物的方法涉及这种中间体与可变取代的被保护的α-氨基苯甲醛的缩合。

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