- Oxodihydropyridazine derivative and application thereof in antitumor drugs
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The invention belongs to the technical field of drugs, and particularly relates to an oxodihydropyridazine derivative and application thereof in antitumor drugs. MTT results show that the oxodihydropyridazine derivative has the advantage of strong antitumor activity, and can be used for preparing antitumor drugs.
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Paragraph 0021-0023
(2020/07/21)
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- Oxodihydropyridazine derivative and application thereof in antitumor drugs
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The invention belongs to the technical field of medicines, and particularly relates to oxodihydropyridazines and application thereof in antitumor drugs. MTT results show that the oxodihydropyridazinederivative has the advantage of high antitumor activity, and can be used for preparing antitumor drugs.
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Paragraph 0019; 0021; 0022; 0023
(2020/08/29)
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- Discovery of [1,2,4]triazolo[4,3-a]pyrazine derivatives bearing a 4-oxo-pyridazinone moiety as potential c-Met kinase inhibitors
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Two series of [1,2,4]triazolo[4,3-a]pyrazine derivatives bearing 4-oxo-pyridazinone moieties (compounds21a-land22a-l) were designed and their IC50values were evaluated against three cancer cell lines (A549, MCF-7 and HeLa) and c-Met kinase. Among them, the compound with most potential,22i,exhibited excellent anti-tumor activity against A549, MCF-7 and HeLa cancer cell lines with IC50values of 0.83 ± 0.07 μM, 0.15 ± 0.08 μM and 2.85 ± 0.74 μM, respectively, and it also possessed superior c-Met kinase inhibition ability at the nanomolar level (IC50= 48 nM). Moreover, dose-dependent experiments, AO fluorescence staining, cell cycle assay, Annexin V-FITC/PI staining and docking studies were carried out in this study. The results demonstrated that compound22icould be a potential c-Met kinase inhibitor.
- Liu, Xiaobo,Sun, Xin,Xiong, Hehua,Xu, Shan,Yang, Zunhua,Zhang, Binliang,Zhang, Qian,Zheng, Pengwu,Zhu, Wufu
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p. 9053 - 9063
(2020/06/08)
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- Design, synthesis and biological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing pyridazinone moiety as c-Met Inhibitors
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Deregulation of the receptor tyrosine kinase mesenchymal epithelial transition factor (MET) has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, a series of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing pyridazinone derivatives were designed, synthesized and evaluated for their enzymatic inhibitory activity against c-Met kinase and cellular potency against A549, HepG2, and MCF-7 cell lines. Eight of them are equal to more active than positive control Foretinib against one or more cell lines and enzyme. The most promising compound 53 showed superior activity to Foretinib, which possessed excellent c-Met kinase inhibition on a singledigital nanomolar level (IC50 = 0.6 nM), and cancer cells of A549 (IC50 = 0.003 μM), HepG2 (IC50 = 0.49 μM) and MCF-7 cells (IC50 = 0.006 μM). The result of AO single staining indicated that compound 53 could induce remarkable apoptosis of HepG2 cell.
- Liu, Xiaobo,Kou, Jianlan,Xiao, Zhen,Tian, Fajuan,Hu, Jiayi,Zheng, Pengwu,Zhu, Wufu
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- A facile and rapid synthesis of benzothiazines
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A series of 2H. 4H-2-[3-methyl-4-(substituted) phenyl azo pyrazolon-5-one-1-yl]-carbonyl methyl-3-oxo-1,4-benzothiazines have been synthesized by the reaction of 2H, 4H-2-hydrazino carbonyl methyl-3-oxo-1,4- benzothiazine with substituted acetoacetic ester derivatives using ultrasound and microwave irradiation. All the synthesized compounds were investigated for their antibacterial activities. The result indicated that the compounds showed convincing activities against Gram-positive bacteria (Bacillus subtilis and Streptococcus lactis) when compared with standard drug (ampicillin trihydrate). These compounds were also synthesized by conventional method and their structures have been elucidated on the basis of spectral analyses and chemical analysis.
- Dabholkar, Vijay V.,Gavande, Rahul P.
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p. 365 - 368
(2013/09/24)
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- Synthesis of 5-(substituted phenylazo)-6-hydroxy-4-methyl-3--cyano-2- pyridones from ethyl 3-oxo-2-(substituted phenylazo)butanoates
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A new procedure for the synthesis of known azo pyridone dyes is presented. A series of 5-(substituted arylazo)-6-hydroxy-4-methyl-3-cyano-2--pyridones were prepared from ethyl 3-oxo-2-(substituted phenylazo)butanoates and cyanoacetamide in acetone using potassium hydroxide as a catalyst by simple refluxing the reaction mixture. The structure of these dyes was confirmed by FT-IR, NMR and UV-Vis spectroscopy. Copyright 2011 (CC) SCS.
- Dostanic, Jasmina,Valentic, Natasa,Uscumlic, Gordana,Mijin, Dusan
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experimental part
p. 499 - 504
(2012/02/03)
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- Some Transition Metal Complexes Derived from the Heterocyclic Ligands 3-Methyl-4-Arylazopyrazole-5-Ones
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Some planar and octahedral complexes of the sulphates of Cu(II) and Ni(II) with different 3-methyl-4-arylazo pyrazole-5-ones have been prepared.The complexes contain only one molecule of the ligand which functions as a bidentate donar coordinating through its carbonyl and azo group while the rest of the positions in the coordination geometry of metal are occupied by water molecules.The magnetic and electronic data of the complexes are discussed in the light of structures assigned.
- Shukla, P. R.,Srivastava, Chandreshwari
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p. 937 - 939
(2007/10/02)
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