高等学校化学学报
高等學校化學學報
고등학교화학학보
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES
2013年
7期
1646-1652
,共7页
彭俊梅%李婉%申坤%霍素芳%叶姣%胡艾希
彭俊梅%李婉%申坤%霍素芳%葉姣%鬍艾希
팽준매%리완%신곤%곽소방%협교%호애희
5-苄基-4-叔丁基-2-芳氨基噻唑%合成%抗肿瘤活性
5-芐基-4-叔丁基-2-芳氨基噻唑%閤成%抗腫瘤活性
5-변기-4-숙정기-2-방안기새서%합성%항종류활성
5-Benzyl-4-tert-butyl-N-arylthiazol-2-amine hydrobromide%Synthesis%Antitumor activity
以芳香胺和4,4-二甲基-1-芳基-2-溴戊-3-酮为原料,设计合成了29种新的5-苄基-4-叔丁基-2-芳氨基噻唑氢溴酸盐化合物；其结构经1H NMR和元素分析等确证.体外抗肿瘤活性测试结果表明,化合物A4,A5,A12和A29对人非小细胞肺癌细胞A549的IC50值分别为0.016,0.019,0.019和0.026 μmol/mL,与阳性对照物紫杉醇(ICso值为0.022 μmol/mL)相当；化合物A5,A7,A13,A14和A19对肝癌细胞Bel7402的IC50值分别为0.021,0.021,0.026,0.014和0.029μmol/mL,与阳性对照物紫杉醇的IC50值(0.030μmol/mL)相近.利用倒置显微镜和Hoechst33342-PI双染色法观察了细胞经化合物处理后的形态变化.
以芳香胺和4,4-二甲基-1-芳基-2-溴戊-3-酮為原料,設計閤成瞭29種新的5-芐基-4-叔丁基-2-芳氨基噻唑氫溴痠鹽化閤物；其結構經1H NMR和元素分析等確證.體外抗腫瘤活性測試結果錶明,化閤物A4,A5,A12和A29對人非小細胞肺癌細胞A549的IC50值分彆為0.016,0.019,0.019和0.026 μmol/mL,與暘性對照物紫杉醇(ICso值為0.022 μmol/mL)相噹；化閤物A5,A7,A13,A14和A19對肝癌細胞Bel7402的IC50值分彆為0.021,0.021,0.026,0.014和0.029μmol/mL,與暘性對照物紫杉醇的IC50值(0.030μmol/mL)相近.利用倒置顯微鏡和Hoechst33342-PI雙染色法觀察瞭細胞經化閤物處理後的形態變化.
이방향알화4,4-이갑기-1-방기-2-추무-3-동위원료,설계합성료29충신적5-변기-4-숙정기-2-방안기새서경추산염화합물；기결구경1H NMR화원소분석등학증.체외항종류활성측시결과표명,화합물A4,A5,A12화A29대인비소세포폐암세포A549적IC50치분별위0.016,0.019,0.019화0.026 μmol/mL,여양성대조물자삼순(ICso치위0.022 μmol/mL)상당；화합물A5,A7,A13,A14화A19대간암세포Bel7402적IC50치분별위0.021,0.021,0.026,0.014화0.029μmol/mL,여양성대조물자삼순적IC50치(0.030μmol/mL)상근.이용도치현미경화Hoechst33342-PI쌍염색법관찰료세포경화합물처리후적형태변화.
