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新型汉防己甲素衍生物的合成及其生物活性
卫笑;杨义芳;赵正保
【期刊名称】《合成化学》 【年(卷),期】2016(024)003
【摘 要】Six novel tetrandrine derivatives(4a~4f) were synthesized by Suzuki coupling reaction of boronic acid derivatives and 5-bromotetrandrine, which was obtained by bromination, using tetrandrine as the starting material.The structures were characterized by 1 H NMR, 13 C NMR and ESI-MS.The in-hibition activities of 4 a~4 f against A549 and HL60 cancer cell lines were investigated by CCK-8 as-say.The compounds which had better inhibition activities were secondary screened by MTT assay.The inhibitory activities of 4a~4f against PTKs were tested by ELISA.The results showed that 4b, 4c and 4e exhibited well inhibition activities against the two cancer cell lines.4b and 4c showed better inhibi-tion activities against FGFR1.%以汉防己甲素为原料,经溴代反应制得关键中间体5-溴汉防己甲素(2);2与硼酸衍生物经Suzuki反应合成了6个新型的汉防己甲素衍生物(4a~4f),其结构经1H NMR,13C NMR和ESI-MS表征。采用CCK-8法初步考察了4a~4f对人早幼粒白血病细胞(HL60)和人肺癌细胞(A549)的抑制活性;并采用MTT法对活性较好的化合物进行复筛。采用酶联免疫吸附法考察4a~4f对多种受体酪氨酸激酶的抑制活性。结果表明:4b,4c和4e对HL60和A549有一定的抑制活性;4b和4c对受体酪氨酸激酶FGFR1的抑制活性大于50%。
【总页数】6页(P192-197) 【作 者】卫笑;杨义芳;赵正保
【作者单位】山西医科大学药学院,山西太原 030001;上海医药工业研究院,上海 200040;山西医科大学药学院,山西太原 030001 【正文语种】中 文
【中图分类】O621.3;O625.1 【相关文献】
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