伊马替尼类似物及冬凌草甲素衍生物的合成与活性研究

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第一部分:伊马替尼类似物的合成与活性研究甲磺酸伊马替尼作为第一个分子靶向治疗的抗肿瘤药物,在治疗慢性粒细胞性白血病上取得了巨大成功。但是随着临床应用范围的扩大和时间的推移,其治疗费用昂贵及耐药现象也逐渐显现。为了开发新型的BCR-ABL激酶抑制剂,本课题通过药物化学合理设计和Discovery Studio药物发现平台的辅助,我们设计了12种结构全新、未见报道的伊马替尼类似物。应用慢性粒细胞白血病细胞株K562,对类似物的活性做了检测,发现在12种类似物中,PAP
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