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    • 8. 发明授权
    • Quinazoline derivatives and quinazoline complex protein kinase inhibitor for inhibiting multiplication of tumor cells and preparation method thereof
    • 喹唑啉衍生物和喹唑啉复合蛋白激酶抑制剂抑制肿瘤细胞增殖及其制备方法
    • US09233995B2
    • 2016-01-12
    • US13882100
    • 2011-10-27
    • Fuyi WangQun LuoLiyun JiWei ZhengShuang LvXianchan Li
    • Fuyi WangQun LuoLiyun JiWei ZhengShuang LvXianchan Li
    • C07F15/00C07D239/94C07D403/12C07F17/02
    • C07F15/0053C07D239/94C07D403/12C07F15/0046C07F17/02
    • Quinazoline derivatives represented by general formula (1) and quinazoline complexes as protein kinase inhibitors, and their preparation methods are provided. Wherein, in general formula (1), at least one of R and R′ is a group containing an atom capable of coordinating with noble metals, m and n are either the same or different and are integers from 0 to 5. Said quinazoline complex as protein kinase inhibitor is formed by coordination compound containing noble metal and said quinazoline derivative ligand capable of coordinating with noble metal in the coordination compound. Used as tyrosine protein kinase inhibitors, Quinazoline derivatives and quinazoline complexes as protein kinase inhibitors provided by the present invention have exhibited good inhibitory effect on proliferation of various tumor cells including human breast cancer cells line (drug-resistant) MCF-7/A, human breast cancer cell line (sensitive) MCF-7/S, prostate cancer cell PC-3, keratinocytes Colo-16, human non-small cell lung cancer cell line A549, etc.
    • 提供了由通式(1)表示的喹唑啉衍生物和喹唑啉配合物作为蛋白激酶抑制剂及其制备方法。 其中,在通式(1)中,R和R'中的至少一个是含有与贵金属配位的原子的基团,m和n可以相同或不同,为0〜5的整数。所述喹唑啉络合物 因为蛋白激酶抑制剂是由含有贵金属的配位化合物和能与配位化合物中的贵金属配位的喹唑啉衍生物配体形成的。 作为酪氨酸蛋白激酶抑制剂,本发明提供的蛋白激酶抑制剂喹唑啉衍生物和喹唑啉配合物对包括人乳腺癌细胞系(耐药性)MCF-7 / A,人类在内的各种肿瘤细胞的增殖具有良好的抑制作用 乳腺癌细胞株(敏感)MCF-7 / S,前列腺癌细胞PC-3,角质形成细胞Colo-16,人非小细胞肺癌细胞株A549等