复杂不饱和异甜菊醇衍生的三唑共轭物的合成与抗癌评估
Synthesis and anticancer evaluation of complex unsaturated isosteviol-derived triazole conjugates.
作者信息
Khaybullin Ravil N, Liang Xiao, Cisneros Katherine, Qi Xin
机构信息
Department of Medicinal Chemistry, College of Pharmacy, University of Florida, Gainesville, FL 32610, USA.
出版信息
Future Med Chem. 2015;7(18):2419-28. doi: 10.4155/fmc.15.158. Epub 2015 Dec 11.
Abstract
BACKGROUND
For the last two decades, diterpenoid isosteviol and its derivatives have gained significant attention for novel chemical transformation in the drug discovery field.
RESULTS
An efficient way towards the synthesis of structurally diverse isosteviol derivatives was described here employing unsaturated functionalities as attractive templates for further transformation such as epoxidation. These structurally diverse compounds exhibited promising cytotoxic activities on different types of cancer cell lines, leading to drug discovery derived from natural products for the treatment of cancer.
CONCLUSION
In this work, novel isosteviol derivatives with Michael acceptors were synthesized to expand the diversity and complexity of a class of isosteviol-derived triazole conjugates to facilitate the development of potential antitumor agents.
摘要
背景
在过去二十年中，二萜类化合物异甜菊醇及其衍生物在药物发现领域的新型化学转化方面受到了广泛关注。
结果
本文描述了一种高效合成结构多样的异甜菊醇衍生物的方法，该方法利用不饱和官能团作为进一步转化（如环氧化）的有吸引力的模板。这些结构多样的化合物在不同类型的癌细胞系上表现出有前景的细胞毒性活性，从而推动了源自天然产物的抗癌药物发现。
结论
在这项工作中，合成了具有迈克尔受体的新型异甜菊醇衍生物，以扩大一类异甜菊醇衍生的三唑共轭物的多样性和复杂性，促进潜在抗肿瘤药物的开发。
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