57800-76-7Relevant academic research and scientific papers
Discovery of 3-(thiophen/thiazole-2-ylthio)pyridine derivatives as multitarget anticancer agents
Zhang, Jiankang,Xi, Jianjun,He, Ruoyu,Zhuang, Rangxiao,Kong, Limin,Fu, Liping,Zhao, Yanmei,Zhang, Chong,Zeng, Linghui,Lu, Jingyi,Tao, Rujia,Liu, Zhengmengtong,Zhu, Huajian,Liu, Shourong
, p. 1633 - 1647 (2019/07/30)
A series of novel 3-(thiophen/thiazole-2-ylthio)pyridine derivatives were designed and synthesized as IGF-1R tyrosine kinase inhibitors. All the target compounds were tested for their IGF-1R kinase inhibitory activities and cytotoxicities against five cancer cell lines (K562, Hep-G2, HCT-116, WSU-DLCL2, and A549). Although all these compounds exhibited moderate to potent cancer cell proliferation inhibitory activities (the most potent compound 43 showed IC50 value of 1.3 ± 0.9 μM against WSU-DLCL2 cell line), IGF-1R inhibition were not observed. In order to identify the exact target of these analogues, selected compounds were further screened for various kinases. The results indicated that this series of compounds may exert their anticancer activities through inhibiting various kinases including FGFR 3, EGFR, JAK, and RON. In addition, cell cycle analysis of compound 43 on Hep-G2 cells showed cell cycle arrest at G1/G0 phase. All the experiments validated the potential of 3-(thiophen/thiazole-2-ylthio)pyridine analogues as multi-target anticancer agents.
BUMETANIDE DERIVATIVES FOR THE THERAPY OF HYPERHIDROSIS
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, (2019/10/30)
The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of diseases/disorders involving Na+- K+- 2CI- - cotransporters (NKCCs), and particularly for use in the treatment or prevention of hyperhidrosis.
Biaryl pyridine deubiquitinating enzyme inhibitor as well as preparation method and application thereof
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, (2018/05/01)
The invention designs and synthesizes a biaryl pyridine deubiquitinating enzyme inhibitor. The biaryl pyridine deubiquitinating enzyme inhibitor has the structure which is shown as a general formula (I). The biaryl pyridine deubiquitinating enzyme inhibit
HETEROCYCLIC DERIVATIVES AND USE THEREOF
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Page/Page column 114, (2015/01/06)
A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.
5-5-MEMBERED FUSED HETEROCYCLIC COMPOUND AND USE THEREOF AS HCV POLYMERASE INHIBITOR
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Page/Page column 122, (2008/06/13)
The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and
