65996-60-3

Upstream product

• 62-53-3 aniline 
• 4949-44-4 ethyl propanoylacetate 
• 5462-33-9 ethyl phenylazoacetoacetate 
• 141-97-9 ethyl acetoacetate 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 10475-63-5 3-oxo-2-(phenylhydrazono)butyric acid ethyl ester 

Downstream Products

• 147920-37-4 4-oxo-1-phenyl-1,4-dihydropyridazine-3-carboxylic acid 

Relevant academic research and scientific papers

Preparation method and application of compound containing zinc-bound and quinoline skeleton

The invention relates to the field of pharmaceutical chemistry, in particular to a novel zinc-containing binding group-containing quinoline compound. A geometric isomer, a pharmaceutically acceptable salt, solvate or prodrug thereof, a preparation method and thereof, and a pharmaceutical composition containing the compound. The invention also relates to an application of the compound in preparation of drugs for treating and/or preventing diseases mediated by c-Met tyrosine kinase and HDAC. The quinoline compounds, geometric isomers and pharmaceutically acceptable salts, solvates and prodrugs thereof are shown in the specification, and R. 1 , m, Q, X, As described in the claims and the description.

Oxodihydropyridazine derivative and application thereof in antitumor drugs

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.

Discovery of Novel c-Mesenchymal-Epithelia transition factor and histone deacetylase dual inhibitors

Clinically, a single agent that simultaneously inhibits multiple targets has been widely used in cancer treatment to overcome complicated dose design and anti-cancer resistance. Inspired by the synergistic effects between c-Met and HDAC in tumor developme

Oxodihydropyridazine derivative and application thereof in antitumor drugs

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.

Discovery of [1,2,4]triazolo[4,3-a]pyrazine derivatives bearing a 4-oxo-pyridazinone moiety as potential c-Met kinase inhibitors

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.

Triazolo pyrazine compound containing heteroaryl substituted pyridazinone structure, and preparation method and applications thereof

The invention relates to a triazolo pyrazine compound containing a heteroaryl substituted pyridazinone structure, and pharmaceutically acceptable salts, hydrates, solvates, and a prodrug thereof, wherein the triazolo pyrazine compound containing a heteroa

Synthesis and bioevaluation study of novel N-methylpicolinamide and thienopyrimidine derivatives as selectivity c-Met kinase inhibitors

Four series of N-methylpicolinamide moiety and thienopyrimidine moiety bearing pyridazinone were designed and synthesized and evaluated for the IC50 values against three cancer cell lines (A549, HepG2 and MCF-7) and some selected compounds were

Design, synthesis and biological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives bearing pyridazinone moiety as c-Met Inhibitors

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.

Discovery of novel pyrrolo-pyridine/pyrimidine derivatives bearing pyridazinone moiety as c-Met kinase inhibitors

In continue to our previous research, eight series of pyrrolo[2,3-b]pyridine and pyrrolo[2,3-d]pyrimidine derivatives bearing pyridazinone moiety were designed, synthesized, and the in vitro antitumor activity was evaluated against four cancer cell lines (A549, HepG2, MCF-7 and PC-3). Some selected compounds (22f, 22g, 26c and 26e) were evaluated for the activity against c-Met kinase, and according to the results of kinase inhibitory activity, the compound 22g was further evaluated for other four tyrosine kinases (Flt-3, VEGFR-2, c-Kit and EGFR) to test the enzyme-based selectivity. The most promising compound 22g showed excellent activity than lead compound Foretinib against A549, HepG2, MCF-7 and PC-3 cell lines, with the IC50 values of 2.19 ± 0.45 μM, 1.32 ± 0.26 μM, 6.27 ± 1.04 μM and 4.63 ± 0.83 μM. The structure–activity relationships (SARs) and docking studies indicated that the pyrrolo[2,3-b]pyridine derivatives bearing 4-oxo-pyridazinone moiety was superior to the pyrrolo[2,3-d]pyrimidine derivatives bearing 6-oxo-pyridazinone moiety. What's more, the target compounds modified with X and Y (X = H, Y = H) were favorable to the activity. And electron drawing groups (EWGs) of 4-Cl-3CF3 on the aryl group show the best activity.