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;邵薇;何谷;成丽;郭丽;
Author:
收稿日期: 年卷(期)页码:2014,29(01):-1-4
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:3-氨基苯甲酰胺衍生物;合成;抗肿瘤
Key words:
基金项目:国家自然科学基金资助项目(批准号:81001357)
中文摘要
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。
英文摘要
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