Pavan Kumar Ch, Devi A, Ashok Yadav P, Rao Vadaparthi R, Shankaraiah G, Sowjanya P, Jain Nishant, Suresh Babu K
a Division of Natural Products Chemistry , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
b Centre for Chemical Biology , CSIR-Indian Institute of Chemical Technology , Hyderabad 500 607 , India.
J Asian Nat Prod Res. 2016 Nov;18(11):1063-78. doi: 10.1080/10286020.2016.1193012. Epub 2016 Jun 22.
As part of pharmacological-phytochemical integrated studies on medicinal plants from Indian flora, costunolide (1) and dehydrocostus lactone (2), were isolated as major phytochemicals from Saussurea lappa, a plant traditionally used in different Asian systems of medicine. A series of 1,4-disubstituted-1,2,3-triazoles conjugates were synthesized through diastereo selective Michael addition followed by regioselective Huisgen 1,3-dipolar cycloaddition reactions. All these triazolyl derivatives (5a-5j) & (7a-7j) were well characterized using modern spectroscopic techniques and evaluated for their anticancer activity against a panel of five human cancerous celllines. The results indicated that all the analogs displayed moderate cytotoxic activity.
作为对印度植物区系药用植物进行药理-植物化学综合研究的一部分，从木香（一种传统上用于不同亚洲医学体系的植物）中分离出木香烯内酯（1）和脱氢木香内酯（2）作为主要植物化学成分。通过非对映选择性迈克尔加成反应，随后进行区域选择性惠斯根1,3-偶极环加成反应，合成了一系列1,4-二取代-1,2,3-三唑共轭物。所有这些三唑基衍生物（5a - 5j）和（7a - 7j）都使用现代光谱技术进行了充分表征，并针对一组五种人类癌细胞系评估了它们的抗癌活性。结果表明，所有类似物均表现出中等细胞毒性活性。
