23163-86-2Relevant articles and documents
Substituted pyridine-2-formamide compound and application thereof
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Paragraph 0216; 0217-0219, (2020/07/15)
The invention belongs to the technical field of medicinal chemistry, and relates to a substituted pyridine-2-formamide compound and application thereof, wherein specifically the substituted pyridine-2-formamide compound has a structure represented by a formula I. According to the invention, based on excellent in vitro inhibition activity on VEGFR-2 kinase and PDGFR-beta kinase and HUVEC cell inhibition activity, the compound can be used as a small-molecular tyrosine kinase (especially Raf kinase) inhibitor, has the effect of inhibiting cell proliferation and angiogenesis, has good antitumor activity, and has a good effect of treating tumor diseases of mammals (including human beings).
Design and discovery of thioether and nicotinamide containing sorafenib analogues as multikinase inhibitors targeting B-Raf, B-RafV600E and VEGFR-2
Sun, Shaofeng,He, Zuopeng,Huang, Mindong,Wang, Ningning,He, Zongzhong,Kong, Xiangkai,Yao, Jianwen
, p. 2381 - 2391 (2018/04/11)
New sorafenib derivatives containing thioether and nicotinamide moiety were designed and synthesized as B-Raf, B-RafV600E and VEGFR-2 multikinase inhibitors. Their in vitro enzymatic inhibitory activities against B-Raf, B-RafV600E and VEGFR-2 and their antiproliferative activities against HCT-116 and B16BL6 cell lines were evaluated and described. Most of the compounds showed potent activities against both cell lines and specific kinases. Compounds a1, b1 and c4, which exhibited the most potent inhibitory activities against B-Raf with IC50 of 21 nM, 27 nM and 17 nM, B-RafV600E with IC50 of 29 nM, 28 nM and 16 nM, VEGFR-2 with IC50 of 84 nM, 46 nM and 63 nM, respectively, and good antiproliferative activities, also demonstrated competitive antiangiogenic activities to sorafenib in in vitro HUVEC tube formation assay.
A block containing nicotinamide diphenyl thiourea compound and its salt preparation method and use of
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Paragraph 0083-0085, (2017/08/02)
The invention relates to a diphenyl thiourea compound containing niacinamide building blocks and salt of the diphenyl thiourea compound. The chemical structure of the diphenyl thiourea compound is as shown in the description. The diphenyl thiourea compound and the salt, pharmaceutically acceptable, of the diphenyl thiourea compound have inhibiting effects on various tumour cell strains and can serve as effective components for preparing tumour treatment medicine.