Design and synthesis of novel D-ring fused steroidal heterocycles

Design and synthesis of novel D-ring fused steroidal heterocycles
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新型D环稠合甾族杂环化合物的设计与合成

DOI:
10.1016/j.steroids.2013.07.006
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发表时间:
2013-12-11
期刊:
影响因子:
2.7
通讯作者:
Liu, Hong-Min
Liu, Hong-Min
中科院分区:
医学3区
文献类型:
--
作者:
Zhang, Bao-Le;Zhang, En;Liu, Hong-Min

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我们以脱氢表雄酮为原料,合成了一系列具有d环并与杂环融合的类固醇类似物,它们是吡啶、咪唑[2,1-b]噻唑或取代噻唑亚胺。所有的最终结构都是首次报道并通过核磁共振和质谱鉴定的,这些产物的产率是中等到良好的,反应条件温和。研究了合成的化合物对EC-109(人食管癌)、EC-9706(人食管癌)、MGC-803(人胃癌)的细胞毒性。(C) 2013爱思唯尔公司版权所有。
Using dehydroepiandrosterone as the starting material, we have synthesized a series of steroid analogs possessing a D-ring fused with heterocycles which are pyridine, imidazo [2,1-b]thiazoles or substituted thiazole imines. All the final structures are first reported and identified by NMR and MS spectroscopys, the yields of these products are moderate to good and the reaction conditions are mild. The cytotoxicity of the synthesized compounds against EC-109(human esophageal carcinoma), EC-9706(human esophageal carcinoma), MGC-803(human gastric carcinoma) were investigated. (C) 2013 Elsevier Inc. All rights reserved.