Identification of novel N1-(2-aryl-1, 3-thiazolidin-4-one)-N3-aryl ureas showing potent multi-tyrosine kinase inhibitory activities.
Identification of novel N1-(2-aryl-1, 3-thiazolidin-4-one)-N3-aryl ureas showing potent multi-tyrosine kinase inhibitory activities.
复制标题
新型 N1-(2-芳基-1, 3-噻唑烷-4-酮)-N3-芳基脲的鉴定，显示出有效的多酪氨酸激酶抑制活性。
DOI：
10.1016/j.ejmech.2018.01.061
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发表时间：
2018
影响因子：
6.7
通讯作者：
Fachang Wei
中科院分区：
文献类型：
--
作者：
Baohui Qi;Ying Yang;Huan He;Xupeng Yue;Yuting Zhou;Xing Zhou;Yuyin Chen;Min Liu;Anmian Zhang;Fachang Wei
设计、合成了29个含N1-(2-芳基-1，3-噻唑烷-4-酮)-N3-芳基脲的新化合物，并对其生物活性进行了评价。同时阐明了这一系列化合物的构效关系(SARS)和结合模式。化合物29b对多种酪氨酸激酶包括RON、c-Met、c-Kit、KDR、Src和IGF-1R等具有较强的抑制作用。在体外，化合物29b对A549癌细胞的抑制作用和细胞毒性经IncuCyte活细胞成像证实。
A total of 29 novel compounds bearingN1-(2-aryl-1, 3-thiazolidin-4-one)-N3-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. Compound29bwas identified possessing high potency against multi-tyrosine kinases including Ron, c-Met, c-Kit, KDR, Src and IGF-1R, etc.In vitroantiproliferation and cytotoxicity of compound29bagainst A549 cancer cell line were confirmed by IncuCyte live-cell imaging.
影响因子：
7.3
作者：
Takasu, Kiyosei;Pudhom, Khanitha;Ihara, Masataka
通讯作者：
Ihara, Masataka
影响因子：
56.9
作者：
Engelman, Jeffrey A.;Zejnullahu, Kreshnik;Janne, Pasi A.
通讯作者：
Janne, Pasi A.