N-4-羟基苯基维甲酰胺与呋咱氮氧化物偶联物的合成及抗肿瘤活性研究  

Studies on Synthesis and Anti-tumor Activity of Conjugates of Furoxans to N-(4-Hydroxyphenyl)retinamide

作　　者：郝北辰[1] 张奕华[1] 赖宜生[1] 袁胜涛[2] 张陆勇[2] 

机构地区：[1]中国药科大学新药研究中心,南京210009 [2]中国药科大学新药筛选中心,南京210009

出　　处：《有机化学》2007年第5期629-635,共7页Chinese Journal of Organic Chemistry

摘　　要：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.To search for potential anti-breast cancer drugs, coupling N-（4-hydroxyphenyl）retinamide （4-HPR） with NO donor furoxans through esterification or amidation, a series of NO-donating retinoids were designed and synthesized, and their structures were established by MS, IR, 1H NMR spectra and elemental analysis. The total yield was 8.8%- 12.9%. The anti-breast cancer activities of these target compounds were tested in vitro. Preliminary biological activity test indicated that all target compounds showed anti-tumor effects to a certain degree, among which compound 8g was as potent as anti-tumor drug adriamycin.

关 键 词：合成 一氧化氮供体 维甲酸类化合物 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学] R73-3[医药卫生—药学]