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合成了18个N-苄氧羰基保护的4-取代氨基酸酰胺基-4-脱氧-4′-去甲基表鬼臼毒素衍生物。它们在体外试验中显示出良好的抗L1210白血病细胞(IC502.7×10-1~4.0×10-4mg/L)和KB细胞的活性,部分新化合物的抗L1210和KB细胞的活性超过依托泊甙[Etoposide,IC50(L1210)1.0×10-1mg/L]。
Eighteen N-benzyloxycarbonyl protected 4-substituted amino acid amido-4-deoxy-4’-demethylepipodophyllotoxin derivatives were synthesized. They showed good activity in anti-L1210 leukemia cells (IC50 2.7 × 10 -1 ~ 4.0 × 10 -4 mg / L) and KB cells in in vitro experiments, and some of the new compounds were more active against L1210 and KB cells Etoposide, IC50 (L1210) 1.0 × 10-1 mg / L].