3-酰胺苯甲酰胺衍生物的合成及体外抗肿瘤活性的初步研究  

Synthesis and anti- tumor activity research of a novel series of 3- amidebenzamide derivatives

作　　者：李博[1] 邵薇[1] 何谷[2] 成丽[1] 郭丽[1] 

机构地区：[1]四川大学华西药学院,四川成都610041 [2]四川大学生物治疗国家重点实验室,四川成都610041

出　　处：《华西药学杂志》2014年第1期1-4,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81001357)

摘　　要：目的合成一类新型3-酰胺苯甲酰胺衍生物并研究其体外抗肿瘤活性。方法以2-甲基-5-氨基苯甲酸和2-氯-5-氨基苯甲酸等为起始原料,经过氨基Boc保护、羧基形成酰胺、脱保护基、酰化等反应得到目标化合物;采用MTT法在前列腺癌细胞PC-3、人卵巢癌细胞SKOV-3、人结直肠癌细胞HCT116、人肝癌细胞Hep-G2、人恶性黑色素瘤细胞A375、人肺癌细胞A549和慢性髓细胞性白血病细胞K562等细胞株上进行了体外抗肿瘤活性的测试。结果与结论合成了9个新型化合物,并经1HNMR、MS确证了化学结构。初步的体外抗肿瘤活性显示:化合物Ⅳh和Ⅳi显示出对白血病细胞有较好的活性。OBJECTIVE To synthesize a novel series of 3 - amidebenzamide derivatives and to study their anti - tumor activity in vitro. METHODS The target compounds were synthesized from 5 - amino - 2 - methylbenzoie acid and 5 - amino - 2 - ehlorobenzoic acid by protection of 5 - amino using Boc, formation of amide, deprotection and acylation, etc. The anti - tumor activity in vitro of these compounds was studied by MTT assay on prostate carcinoma cells PC - 3, ovarian carcinoma cells SKOV - 3, human coloreetal cancer cells HCT116, human hepatocellular carcinoma cells Hep -G2 ,malignant melanoma cells A375 ,human lung carcinoma cells A549 and human erythroleukemia cells K562. RESULTS and CONCLUSION Nine new compounds were prepared, and the chemical structures were confirmed by 1HNMR and MS. Preliminary anti - tumor activity in vitro displays that compound lVh and IVi exhibited good activity against chronic myelogenous leukemia.

关 键 词：3-氨基苯甲酰胺衍生物 合成 抗肿瘤 

分 类 号：R914[医药卫生—药物化学]