College of Material, Chemistry and Chemical Engineering, Hangzhou Normal University, Hangzhou 310036, China.
Carbohydr Res. 2010 Feb 11;345(3):437-41. doi: 10.1016/j.carres.2009.11.032. Epub 2009 Dec 5.
A series of novel glycosyl thiazol-2-imines (3a-g) have been synthesized regioselectively in good yields from the hydrolysis of thiazol-2(3H)-imine-linked glycoconjugates. The glycosyl thiazol-2-imines were evaluated for their antitumor activity against Hela (cervical carcinoma), HCT-8 (colon carcinoma) and Bel-7402 (liver carcinoma). Among the compounds screened, 1-benzoyl-4-(4-nitrophenyl)-3-beta-D-glucopyranosyl-thiazol-2(3H)-imine (3c) was found to be the most active compound against HCT-8.
一系列新型糖基噻唑-2-亚胺（3a-g）通过噻唑-2（3H）-亚胺连接的糖缀合物的水解反应以高产率区域选择性合成。评估了糖基噻唑-2-亚胺对 Hela（宫颈癌）、HCT-8（结肠癌）和 Bel-7402（肝癌）的抗肿瘤活性。在所筛选的化合物中，发现 1-苯甲酰基-4-（4-硝基苯基）-3-β-D-吡喃葡萄糖基噻唑-2（3H）-亚胺（3c）对 HCT-8 的活性最强。
