【作者】 刘丹； 李晓静； 郑小洲； 盛志成； 霍春芳； 赵临襄；

【Author】 Dan Liu,Xiaojing Li,Xiaozhou Zheng,Zhicheng Sheng,Chunfang Huo,Linxiang Zhao (Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education,Shenyang Pharmaceutical University,Shenyang,110016,P.R.China.)

【机构】 沈阳药科大学基于靶点的药物设计与研究教育部重点实验室；

【摘要】 目的合成一系列2-(E)-取代-苯基亚甲基-6-(N-取代-胺甲基)环己酮/环己醇类化合物提高其抗肿瘤活性。方法以环己酮为原料,经Stork烯胺介导的Aldol反应、胺交换反应和格氏反应得到目标化合物。结果合成了二十个化合物并测试了它们对人白血病细胞HL-60的体外生长抑制活性。结论含有甲磺酰基的化合物4h,4i,4j表现出了较强的抗增殖活性,GI50分别为0.84,1.12和0.86μM。更多还原

【Abstract】 OBJECTIVE A series of 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones(4a-4j) and cyclohexanols(5a-5j) were designed and synthesized to optimize the anti-proliferative activity.METHODS The compounds were obtained by subsequent Stork-Enamize mediated Aldol reaction,amine exchange reaction and Grignard reaction.RESULTS Twenty compounds were synthesized and their growth inhibitions were tested in human leukemia HL-60 cells in vitro.CONCLUSION Compounds 4h,4i,4j,which owned methylsulfonyl group,showed most potent anti-proliferative activity with GI 50 of 0.84,1.12,and 0.86 μM respectively.更多还原