新型4β-[(4-取代)-1,2,3-三唑-1-基]鬼臼毒素作为潜在抗癌药物的研究。
Studies on novel 4beta-[(4-substituted)-1,2,3-triazol-1-yl] podophyllotoxins as potential anticancer agents.
作者信息
Bhat Bilal A, Reddy P Bhaskar, Agrawal Satyam Kumar, Saxena A K, Kumar H M Sampath, Qazi G N
机构信息
Synthetic Chemistry Division, Pharmacology Division, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu-Tawi 180001, India.
出版信息
Eur J Med Chem. 2008 Oct;43(10):2067-72. doi: 10.1016/j.ejmech.2007.09.015. Epub 2007 Sep 29.
A series of 4beta-[(4-substituted)-1,2,3-triazol-1-yl] podophyllotoxin congeners have been designed and synthesized with significant regioselectivity by employing Cu(I) catalyzed 1,3-dipolar cycloaddition reaction of C4beta-azido podophyllotoxin and C4beta-azido-4'-O-demethyl podophyllotoxin with N-prop-2-yn-1-ylanilines. These compounds were evaluated for anticancer activity against a panel of seven human cancer cell lines. It was interesting to note that all the compounds exhibited promising activity especially against SF-295 (CNS), HCT-15 (colon) and 502713 (colon) cell lines. Compound 11e was found to be the most promising in this study.
通过利用C4β-叠氮鬼臼毒素和C4β-叠氮-4'-O-去甲基鬼臼毒素与N-丙-2-炔-1-基苯胺的Cu(I)催化1,3-偶极环加成反应，设计并合成了一系列具有显著区域选择性的4β-[(4-取代)-1,2,3-三唑-1-基]鬼臼毒素类似物。对这些化合物针对一组七种人类癌细胞系的抗癌活性进行了评估。值得注意的是，所有化合物都表现出有前景的活性，尤其是对SF-295（中枢神经系统）、HCT-15（结肠）和502713（结肠）细胞系。在本研究中发现化合物11e是最有前景的。
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