Zhang Fu-Min, Yao Xiao-Jun, Tian Xuan, Tu Yong-Qiang
State Key Laboratory of Applied Organic Chemistry & Department of Chemistry, Lanzhou University, Lanzhou, 730000, PR China.
Molecules. 2006 Nov 2;11(11):849-57. doi: 10.3390/11110849.
A series of new 4beta-5-Fu-substituted 4'-demethylepipodophyllotoxin derivatives were synthesized and evaluated, together with some previously prepared ones, for their cytotoxic activities against four tumor cell lines (HL60, P388, A549 and BEL7402). Three of these compounds exhibited superior in vitro anticancer activity against P388 and A549 than the reference compound etoposide. In addition, the partition coefficients (P) of all the new and previously synthesized derivatives were determined.
合成并评估了一系列新的4β-5-氟尿嘧啶取代的4'-去甲基表鬼臼毒素衍生物，以及一些之前制备的衍生物，考察它们对四种肿瘤细胞系（HL60、P388、A549和BEL7402）的细胞毒性活性。其中三种化合物对P388和A549的体外抗癌活性优于参考化合物依托泊苷。此外，还测定了所有新合成的和之前合成的衍生物的分配系数（P）。
