NO供体型维甲酸类化合物的合成及其对肿瘤细胞增殖的抑制作用  

Synthesis and antitumor activity of NO-donating retinoids

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,江苏南京210009 [2]中国药科大学新药筛选中心,江苏南京210009

出　　处：《中国药物化学杂志》2007年第4期213-216,237,共5页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计合成NO供体型维甲酸类化合物,以期获得对乳腺癌肿瘤细胞的增殖有较好抑制作用的化合物。方法将N-(4-羟基苯基)维甲酰胺(4-HPR)与NO供体呋咱氮-氧化物缩合,合成具有NO释放和诱导乳腺癌细胞凋亡作用的NO供体型维甲酸类化合物;测试目标物体外对乳腺癌肿瘤细胞的增殖抑制作用。结果与结论合成了7个新化合物,其结构经IR、MS和1H-NMR确证。目标物均具有不同程度的抑制肿瘤细胞增殖作用,其中化合物5a、5b、5f、5g对肿瘤细胞的增殖抑制作用较强,值得进一步研究。Aim To design and synthesize new NO-donating retinoid compounds with potential anti-breast cancer activity. Methods A novel class of NO-donating retinoids were synthesized by condensation N-（4-hy- droxyphenyl） retinamide（4-HPR） with NO-donor furoxans. The anti-breast cancer effect of these target compounds were tested in vitro. Results and conclusion Seven new compounds were obtained, their structures were established by MS, IR, ^1H-NMR. Preliminary biological activity test indicate that each target compound exhibit anti-cancer effect to a certain extent, among which, compounds 5a, 5b, 5f, and 5g are worth of further investigation.

关 键 词：一氧化氮供体 维甲酸类化合物 抗乳腺癌活性 

分 类 号：R914[医药卫生—药物化学] R730.5[医药卫生—药学]