具有强效多酪氨酸激酶抑制活性的新型N-(2-芳基-1,3-噻唑烷-4-酮)-N-芳基脲的鉴定
Identification of novel N-(2-aryl-1, 3-thiazolidin-4-one)-N-aryl ureas showing potent multi-tyrosine kinase inhibitory activities.
作者信息
Qi Baohui, Yang Ying, He Huan, Yue Xupeng, Zhou Yuting, Zhou Xing, Chen Yuying, Liu Min, Zhang Anmian, Wei Fachang
机构信息
Department of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai, 519041, Guangdong Province, China.
Department of Bioengineering, Zhuhai Campus of Zunyi Medical University, Zhuhai, 519041, Guangdong Province, China.
出版信息
Eur J Med Chem. 2018 Feb 25;146:368-380. doi: 10.1016/j.ejmech.2018.01.061. Epub 2018 Jan 31.
A total of 29 novel compounds bearing N-(2-aryl-1, 3-thiazolidin-4-one)-N-aryl ureas were designed, synthesized and evaluated for their biological activities. The structure-activity relationships (SARs) and binding modes of this series of compounds were clarified together. Compound 29b was identified possessing high potency against multi-tyrosine kinases including Ron, c-Met, c-Kit, KDR, Src and IGF-1R, etc. In vitro antiproliferation and cytotoxicity of compound 29b against A549 cancer cell line were confirmed by IncuCyte live-cell imaging.
共设计、合成了29种含N-(2-芳基-1,3-噻唑烷-4-酮)-N-芳基脲的新型化合物，并对其生物活性进行了评估。同时阐明了该系列化合物的构效关系（SARs）和结合模式。化合物29b被鉴定为对包括Ron、c-Met、c-Kit、KDR、Src和IGF-1R等多种酪氨酸激酶具有高效活性。通过IncuCyte活细胞成像证实了化合物29b对A549癌细胞系的体外抗增殖和细胞毒性。
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