Reddy Pitta B, Paul David V, Agrawal Satyam K, Saxena Ajit K, Kumar Halmuthur M S, Qazi Ghulam N
Department of Synthetic Chemistry, Indian Institute of Integrative Medicine, Jammu-Tawi, India.
Arch Pharm (Weinheim). 2008 Feb;341(2):126-31. doi: 10.1002/ardp.200700116.
A series of 4beta-[(4-substituted)-1,2,3-triazol-1-yl]podophyllotoxin analogues have been synthesized with high regio-selectivity by employing copper(I)-catalyzed 1,3-dipolar cycloaddition of 1-O-propargyl monosaccharides with C4beta-azido podophyllotoxin and C4beta-azido-4'-O-demethyl podophyllotoxin. All the compounds were evaluated for their anticancer activity against a panel of six human cancer cell lines. Among these, 4'-O-demethyl podophyllotoxin congeners are showing promising anticancer activity mainly against HCT-15 (colon) and DU-145 (prostate) cells.
通过使用铜（I）催化的1-O-炔丙基单糖与C4β-叠氮基鬼臼毒素和C4β-叠氮基-4'-O-去甲基鬼臼毒素的1,3-偶极环加成反应，以高区域选择性合成了一系列4β-[(4-取代)-1,2,3-三唑-1-基]鬼臼毒素类似物。对所有化合物针对六种人类癌细胞系的抗癌活性进行了评估。其中，4'-O-去甲基鬼臼毒素同系物主要对HCT-15（结肠）和DU-145（前列腺）细胞显示出有前景的抗癌活性。
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