Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou 510632, PR China.
Eur J Med Chem. 2011 Jun;46(6):2490-502. doi: 10.1016/j.ejmech.2011.03.038. Epub 2011 Mar 25.
Based on structural modifications of the natural 23-hydroxybetulinic acid, a series of novel its derivatives had been synthesized. The new compounds were screened for in vitro antiproliferative activity against cancer cell lines HeLa, MCF-7, HepG2, B16 and A375 using doxorubicin as a reference. The vast majority of derivatives had exhibited potent tumor growth inhibitory activity than original compound. The derivatives 4, 5, 7, 20, 23, 26, 43 and 44 with IC50 values lower than 10 μM on all tested cell lines were regarded as the most promising compounds. The structure-activity relationships of 23-hydroxybetulinic acid derivatives were also discussed in the present investigations.
基于天然 23-羟基白桦酸的结构修饰，我们合成了一系列新型衍生物。这些新化合物在体外针对癌细胞系 HeLa、MCF-7、HepG2、B16 和 A375 的抗增殖活性进行了筛选，以阿霉素作为参比。与原始化合物相比，绝大多数衍生物都表现出更强的肿瘤生长抑制活性。衍生物 4、5、7、20、23、26、43 和 44 在所有测试的细胞系中，IC50 值均低于 10 μM，被认为是最有前途的化合物。本研究还讨论了 23-羟基白桦酸衍生物的构效关系。
