微波促进新型噁嗪酮类化合物的合成及抗肿瘤活性初筛  

Microwave promotes synthesis of new oxazine ketones and their antitumor activity screening

作　　者：徐应淑 叶金雄 杨成莉 史大斌 陈永正 张磊 Xu Yingshu;Ye Jinxiong;Yang Chengli;Shi Dabin;Chen Yongzheng;Zhang Lei(School of Pharmacy,Zunyi Medical University,Zunyi Guizhou 563099,China)

机构地区：[1]遵义医科大学药学院,贵州遵义563099

出　　处：《遵义医科大学学报》2020年第1期38-40,共3页Journal of Zunyi Medical University

基　　金：贵州省科技厅资助项目(NO:黔科合J字2011[2083])。

摘　　要：目的一类新型噁嗪酮类化合物的合成。方法以5,5-二甲基-1,3-环己二酮、苯甲醛和脂肪伯胺为原料,经过微波促进的Wolff重排和杂Diels-Alder等反应合成目标产物。采用MTT法测试产物对人卵巢癌细胞的抗肿瘤活性。结果合成了3个结构新颖的噁嗪酮类化合物,经1HNMR,13 CNMR和ESI-MS表征确证为目标化合物,MTT法初步测试目标产物对人卵巢癌细胞SKOV-3有一定的抗肿瘤活性,化合物6b的IC 50值为146μg/mL。结论该合成方法可行,同时,目标化合物具有一定的体外抗肿瘤活性。Objective This paper was mainly about the synthesis and characterization of the novel oxazine ketone compounds.Methods The synthesis of target compounds was performed by microwave-assisted Wolff rearrangement and hetero-Diels-Alder reaction using 5,5-dimethyl-1,3-cyclohexanedione,benzaldehyde and alkyl primary amines as starting materials.The anti-tumor activity of target compounds on human ovarian cancer cells was tested by MTT method.Results Three novel oxazinones were synthesized.The structures of target molecules were confirmed by 1HNMR,13CNMR and ESI-MS.Preliminary anticancer activity of target compounds was evaluated against human ovarian cancer cells(SKOV-3)in vitro by MTT assay.Conclusion The results showed the synthesis method was feasible and the target compounds exhibited moderate anti-proliferative activity.

关 键 词：噁嗪酮 合成 微波 生物活性 

分 类 号：TQ450.2[化学工程—农药化工]