796967-48-1Relevant articles and documents
Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors
Sun, Ying,Shan, Yuanyuan,Li, Chuansheng,Si, Ru,Pan, Xiaoyan,Wang, Binghe,Zhang, Jie
, p. 373 - 385 (2017/10/16)
VEGFR-2, TIE-2, and EphB4 are essential for both angiogenesis and tumorigenesis. Herein, we designed and prepared three classes of multi-target inhibitors based on the extensive sequence homology along the kinase domain of angiogenic RTKs. Biological evaluation indicated that these multi-target inhibitors exhibited considerable potential as novel anti-angiogeneic and anticancer agents. Among them, a diaryl thiourea bearing 1H-indazole-3-amine (16a) displayed the most potent RTK inhibition and excellent selectivity. It also showed inhibition on viability of human umbilical vein endothelial cells and anti-proliferation against a broad spectrum of cancer cells. Therefore, 1H-indazole-3-amine could serve as a promising hinge binding group for multi-target inhibitors of VEGFR-2, Tie-2, and EphB4.
Diaryl urea compounds with anti-tumor activity as well as preparation method and application of diaryl urea compounds
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Paragraph 0032; 0033, (2017/08/29)
The invention provides diaryl urea compounds with anti-tumor activity as well as a preparation method and an application of the diaryl urea compounds. A structural formula of the compounds is shown in the specification, wherein R1 represents hydrogen, and R2 represents isopropyl or halogen groups. The compounds have good inhibition activity for VEGFR-2 (vascular endothelial growth factor-2) kinase, and can block VEGFR-2 kinase induced signaling pathways and inhibit tumor cell proliferation and migration by inhibiting activity of VEGFR-2 kinase, so that the compounds can be applied to preparation of anti-tumor drugs. Besides, the preparation method of the compounds has the advantages that raw materials are easily available, reaction conditions are mild, a reaction process is simple to operate and used reagents are cheap.
Diarylurea compound with antitumor activity, and preparation method and application thereof
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, (2017/07/19)
The invention provides a diarylurea compound with antitumor activity, and a preparation method and application thereof. The compound has a structural formula as described in the specification. In the structural formula, R1 and R2 are selected from the group consisting of hydrogen, alkane groups or halogen groups. The compound provided by the invention has good inhibitory activity to VEGFR-2 kinase, so a signal channel induced by the VEGFR-2 kinase can be blocked through inhibition of the activity of the VEGFR-2 kinase, and proliferation and migration of tumor cells are inhibited; thus, the compound can be applied in preparation of antitumor drugs. Meanwhile, the preparation method for the compound has the following advantages: raw materials are easily available; reaction conditions are mild; the process of reaction is simple to operate; and used reagents are cheap.