| Aurora激酶抑制剂的结构优化策略 |
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| 引用本文： | 吉米,姚宏亮,江程,尤启冬. Aurora激酶抑制剂的结构优化策略[J]. 药学进展, 2012, 36(4): 145-151 |
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| 作者姓名： | 吉米 姚宏亮 江程 尤启冬 |
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| 作者单位： | 中国药科大学药物化学教研室,江苏南京,210009 |
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| 基金项目： | 国家自然科学基金(No.30801437) |
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| 摘 要： | Aurora激酶是一种丝氨酸/苏氨酸蛋白激酶,在肿瘤细胞的有丝分裂进程中起着重要的调控作用。因此,以该激酶为靶点,开发新型抗肿瘤药物,已成为研究热点。从提高化合物的活性和选择性、增加其水溶性及改善其药动学性质等方面,综述Aurora激酶抑制剂的结构优化策略。
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| 关 键 词： | Aurora激酶 抑制剂 结构优化 活性 选择性 水溶性 药动学 |
Strategies for the Structure Optimization of Aurora Kinase Inhibitors |
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| LELU KAKILA Jimmy , YAO Hong-liang , JIANG Cheng , YOU Qi-dong. Strategies for the Structure Optimization of Aurora Kinase Inhibitors[J]. Progress in Pharmaceutical Sciences, 2012, 36(4): 145-151 |
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| Authors: | LELU KAKILA Jimmy YAO Hong-liang JIANG Cheng YOU Qi-dong |
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| Affiliation: | (Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing 210009,China) |
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| Abstract: | Aurora kinases,a member of the serine/threonine kinase family,play an important role in the progress of mitosis in tumor cells.Therefore,the development and research of novel anti-tumor agents targeting Aurora kinases are becoming a hotspot.The strategies for the structure optimization of Aurora kinase inhibitors were reviewed from the respects of enhancing their activity and selectivity,increasing their water-solubility and improving their pharmacokinetic profile. |
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| Keywords: | Aurora kinase inhibitor structure optimization activity selectivity water-solubility pharmacokinetic profile |
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