当前位置: X-MOL 学术J. Nat. Prod. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Antineoplastic Agents. 606. The Betulastatins
Journal of Natural Products ( IF 5.1 ) Pub Date : 2018-01-05 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00536
George R. Pettit 1 , Noeleen Melody 1 , Jean-Charles Chapuis 1
Affiliation  

The medicinal potential of the plant pentacyclic triterpene betulin has generated long-term interest focused on various SAR research avenues. The present approach was based on producing further analogues (chimeras) arising from a studied modification of betulin bonded to the Dov-Val-Dil-Dap unit of the powerful anticancer drug dolastatin 10, which provided betulastatins 1 (7b), 2 (11b), 3 (16b), and 4 (18b). Betulastatin 1, 2, and 4 exhibited modest levels of cancer cell growth inhibition against six cancer cell lines. Betulastatin 3 proved to be the most potent cancer cell growth inhibitor (GI50 0.01 μg/mL) and seems worthy of further development, as the presumed mixture of anticancer mechanisms of action may prove to be useful.

中文翻译:

抗肿瘤药。606. Betulastatins

植物五环三萜甜菜碱的药用潜力引起了人们对各种SAR研究途径的长期关注。本方法基于产生进一步的类似物(嵌合体),该类似物是由于研究到的与强力抗癌药物dolastatin 10的Dov-Val-Dil-Dap单元结合的甜菜碱的修饰而产生的,从而提供了betulastatins 1(7b),2(11b) ,3(16b)和4(18b)。Betulastatin 1、2和4对六种癌细胞系表现出中等水平的癌细胞生长抑制作用。证明Betulastatin 3是最有效的癌细胞生长抑制剂(GI 50 0.01μg/ mL),似乎值得进一步发展,因为推测的抗癌作用机制混合物可能被证明是有用的。
更新日期:2018-01-05
down
wechat
bug