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为了寻找治疗乳腺癌的药物,将N-4-羟基苯基维甲酰胺(4-HPR)以乙酸为连接基团通过酯键或酰胺键与NO供体呋咱氮氧化物缀合,合成了NO供体型维甲酸类化合物,共11个新的目标化合物,其结构经IR,MS,1HNMR和元素分析表征,总收率为8.8%～12.9%.对目标物进行体外抗乳腺癌活性测试,结果表明,所有目标物均具有不同程度的抗肿瘤活性,其中8g抗肿瘤活性和对照药阿霉素相当.
In order to find a drug for treating breast cancer, N-4-hydroxyphenyl retinamide (4-HPR) was conjugated to the NO donor furazanone oxynitride through an ester bond or an amide bond using acetic acid as a linking group to synthesize NO donor retinoid compounds, a total of 11 new target compounds, its structure was characterized by IR, MS, 1HNMR and elemental analysis, the overall yield was 8.8% ~ 12.9% .To test the target against breast cancer activity in vitro, The results showed that all the targets have different degrees of anti-tumor activity, of which 8g antitumor activity and control drug doxorubicin quite.