1094332-66-7Relevant articles and documents
Styryl pyridine compound containing pyridine structure, preparation method and application of styryl pyridine compound in preparation of antitumor drugs (by machine translation)
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Paragraph 0021; 0030-0032; 0112; 0120-0122, (2019/09/05)
The invention belongs to the field, and particularly relates to a styryl pyridine compound containing a pyridine structure, a preparation method and an application of the styryl pyridine compound in preparation of anti-tumor drugs, wherein the compound is a compound as shown in the formula I. The compound of the general formula I has good inhibitory activity on non-small cell lung cancer A549 and liver cancer cell HepepepG2, can be used for preparing antitumor drugs, and is especially suitable for cancers, kidney cancer, lung cancer, thyroid cancer, colon cancer and other tumors. (by machine translation)
Discovery of novel picolinamide-based derivatives as novel VEGFR-2 kinase inhibitors: Synthesis,: in vitro biological evaluation and molecular docking
Sun, Wuji,Fang, Shubiao,Yan, Hong
supporting information, p. 1054 - 1058 (2018/06/27)
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive target for cancer therapy. In our effort, a novel series of picolinamide-based derivatives were designed and synthesized as potent and effective VEGFR-2 inhibitors. All the newly prepared compounds were evaluated in vitro for their antiproliferative activity against A549 and HepG2 cell lines. Among the new compounds, 8j and 8l exhibited better activity against both A549 and HepG2 cell lines. Molecular docking was performed to investigate the binding capacity and binding mode with VEGFR-2 (PDB code: 4ASD).
The structure of the amine-containing thiourea compound and its preparation method and application
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Paragraph 0070; 0071; 0072; 0073; 0075, (2017/08/08)
A disclosed thiourea compounds containing an arylamine structure comprises compounds of a general formula I and pharmaceutically acceptable salts. In the general formula I shown in the specification, R1 is selected from H, C1-C8 alkyl, halogens, -CF3, -OCF3, -NO2, -CN, R2O-, -SO2NH2, -NHSO2R3, -NR4R5, -CONR6R7, -COOR8, R9CO- and disubstituted and trisubstituted combinations thereof, R2, R3, R4, R5, R6, R7, R8 and R9 are respectively H or C1-C8 alkyl, L is selected from -NHR10, -NHOR11, -NR12R13, pyrrolidin-1-yl, 4-piperidyl and (4-methyl-1-piperazinyl)methylene, and R10, R11, R12 and R13 are respectively H, C1-C8 alkyl, cycloalkyl or aryl. The compounds have inhibiting effect on multiple tumor cell strains.
Thiourea and thioether derivatives of sorafenib: Synthesis, crystal structure, and antiproliferative activity
Yao, Jianwen,Chen, Jing,He, Zuopeng,Sun, Wei,Fang, Hao,Xu, Wenfang
, p. 3959 - 3968 (2013/07/26)
A series of novel sorafenib derivatives containing diaryl thiourea and thioether, 9a-u, was designed and synthesized, and their antiproliferative activities against HCT116 and MDA-MB-231 cell lines were also evaluated and described. Most compounds exhibited potent antiproliferative activity against HCT116 cells with IC50 = 1.8-80.4 μM. Compounds 9p, 9r, and 9s demonstrated competitive antiproliferative activities to sorafenib, against all two cancer cell lines. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR, and HRMS, and compound 9n was characterized by single-crystal X-ray diffraction. Primary structure-activity relationships (SAR) have also been established.
Design, synthesis and biological activities of thiourea containing sorafenib analogs as antitumor agents
Yao, Jianwen,Chen, Jing,He, Zuopeng,Sun, Wei,Xu, Wenfang
experimental part, p. 2923 - 2929 (2012/07/14)
A novel series of diaryl thiourea containing sorafenib derivatives 9a-t was designed and synthesized. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR and HRMS. Their antiproliferative activities against HCT116 and MDA-MB-231 cell lines, and their inhibitory activities against the phosphorylation of VEGFR were evaluated and described. Some of the compounds showed significant activities against both cell lines and VEGFR. Compounds 9g, 9m, 9o and 9p demonstrated competitive antiproliferative activities to sorafenib, the reference standard, while compounds 9d, 9m, and 9p showed significant inhibitory activities against the phosphorylation of VEGFR.
Design, synthesis and biological activities of sorafenib derivatives as antitumor agents
Yao, Jianwen,He, Zuopeng,Chen, Jing,Sun, Wei,Fang, Hao,Xu, Wenfang
, p. 6549 - 6553,5 (2012/12/12)
A series of novel sorafenib derivatives, 9a-w, was designed and synthesized in high yields using various substituted anilines, and their antiproliferative activities against HCT116, PC-3 and MDA-MB-231 cell lines were also evaluated and described. All compounds exhibited potent antiproliferative activity against HCT116 and PC-3 cells with IC50 = 2.8-52.0 and 2.2-45.6 μM; compounds 9p and 9q demonstrated competitive antiproliferative activities to sorafenib against all three cancer cell lines, the cytotoxicity of compound 9r is more potent than that of sorafenib. Compounds (9g, 9p, 9q and 9r) were chosen for further evaluation of the anti-angiogenesis activity, and showed the inhibition of sprout formation from aortic ring ex vivo. The structures of all the newly synthesized compounds were determined by 1H NMR, 13C NMR and HRMS.
New sorafenib derivatives: Synthesis, antiproliferative activity against tumour cell lines and antimetabolic evaluation
Babic, Zeljka,Crkvencic, Maja,Rajic, Zrinka,Mikecin, Ana-Matea,Kralj, Marijeta,Balzarini, Jan,Petrova, Mariya,Vanderleyden, Jos,Zorc, Branka
experimental part, p. 1124 - 1137 (2012/03/10)
Sorafenib is a relatively new cytostatic drug approved for the treatment of renal cell and hepatocellular carcinoma. In this report we describe the synthesis of sorafenib derivatives 4a-e which differ from sorafenib in their amide part. A 4-step synthetic
