罗丹宁衍生物的合成及抗肿瘤活性  被引量:1

Synthesis and anti-tumor activity of rhodanine derivatives

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作  者:楚小晶[1] 张英[1] 乔春华[1] 敖桂珍[1] 杨圣伟[1] 董燕[1] 

机构地区:[1]苏州大学医学部药学院,苏州215123

出  处:《中国药科大学学报》2013年第2期113-116,共4页Journal of China Pharmaceutical University

基  金:国家"重大新药创制"科技重大专项资助项目(No.2009ZX09103-129);江苏高校优势学科建设工程资助项目;苏州大学大学生创新性实验基金资助项目(No.5731513010)~~

摘  要:在罗丹宁衍生物WL-276的基础上设计并合成一系列新的罗丹宁衍生物,并对这些化合物的抗肿瘤活性进行测定。以氨基酸为原料,经环合和缩合反应,合成了化合物Ⅱ1-4,然后分别与硫化氢供体ADT-OH偶联得到化合物Ⅲ1-4,共合成了8个目标化合物,其中4个未见报道,其结构均经1H NMR、IR和HR-MS确证。然后用MTT法筛选其抗肿瘤活性。初步研究表明,化合物Ⅱ1,3,4和Ⅲ1-4对HepG2肿瘤细胞和DU145肿瘤细胞的增殖均具有较强的抑制作用,且化合物Ⅲ的活性比Ⅱ强;化合物Ⅲ2,4对HepG2细胞和化合物Ⅲ1,2,4对DU145细胞的抗增殖活性均高于阳性对照5-氟尿嘧啶。Based on the study of rhodanine derivative WL-276,some novel compounds were synthesized,and their anti-tumor effects were screened by MTT method.Compounds II1-4 were obtained by cyclization and condensation from the certain amino acids,and then coupled respectively with hydrogen sulfide donor ADT-OH to afford compounds III1-4,whose structures were confirmed by 1H NMR,IR and HR-MS.Furthermore,preliminary pharmacological results suggested that compounds II1,3,4,III1-4 had strong inhibitory effects on the proliferation of HepG2 and DU145 tumor cells.Particularly,the anti-proliferation activity of compounds III2,4 on HepG2 and compounds III1,2,4 on DU145 tumor cells was stronger than that of the positive control,5-fluorouracil.

关 键 词:罗丹宁衍生物 合成 硫化氢供体 抗肿瘤活性 

分 类 号:R914.5[医药卫生—药物化学]

 

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