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4′-去甲表鬼臼毒素与叠氮酸在三氟化硼乙醚存在下缩合,并经还原得4-氨基-4-脱氧-4′-去甲表鬼臼毒素。该中间体与酸或酸酐反应得相应酰胺化合物24个。经体外筛选,多数化合物抑制L_(1210)和KB细胞活性相当或超过依托泊甙。与相应的醚、酯、胺等类型相比,这一类化合物活性最强。
The 4’-norvodipodophyllotoxin is condensed with azido acid in the presence of boron trifluoride diethyl ether and reduced to give 4-amino-4-deoxy-4’-norvodipodophyllotoxin. This intermediate was reacted with acid or anhydride to give 24 corresponding amide compounds. In vitro screening, most compounds inhibit L_ (1210) and KB cell activity comparable or exceed etoposide. Compared with the corresponding ether, ester, amine and other types, this class of compounds is the most active.