Department of Chemistry, Hanshan Normal University, Chaozhou, 521041, China,
Arch Pharm Res. 2013 Dec;36(12):1447-53. doi: 10.1007/s12272-013-0155-x. Epub 2013 May 23.
Ten lupeol dicarboxylic acid monoester derivatives as new potent antitumor agents were synthesized and evaluated for in vitro antitumor activities against A549, LAC, HepG2 and HeLa cell lines. Among them, compounds 1-5 showed excellent antitumor activities against all tested tumor cell lines and compounds 6-10 exhibited high activities against A549, HepG2 and HeLa cells, exceeded lupeol, lupanol and doxorubicin. Compound 2 displayed the highest potent antitumor activities with IC50 values of 5.78 μM against A549 cell, 2.38 μM against LAC cell, 6.14 μM against HepG2 cell and 0.00842 μM against HeLa cell.
合成了 10 个作为新型强效抗肿瘤剂的羽扇豆醇二羧酸单酯衍生物，并对其进行了体外抗肿瘤活性评估，针对 A549、LAC、HepG2 和 HeLa 细胞系。其中，化合物 1-5 对所有测试的肿瘤细胞系均表现出优异的抗肿瘤活性，化合物 6-10 对 A549、HepG2 和 HeLa 细胞表现出高活性，超过了羽扇醇、羽扇豆醇和阿霉素。化合物 2 显示出最高的抗肿瘤活性，其对 A549 细胞的 IC50 值为 5.78 μM，对 LAC 细胞的 IC50 值为 2.38 μM，对 HepG2 细胞的 IC50 值为 6.14 μM，对 HeLa 细胞的 IC50 值为 0.00842 μM。
