286371-71-9

Upstream product

• 123-30-8 4-amino-phenol 
• 13790-39-1 6,7-dimethoxy-4-chloroquinazoline 
• 5653-40-7 2-Amino-4,5-dimethoxybenzoic acid 
• 100-02-7 4-nitro-phenol 
• 35654-56-9 6,7-dimethoxy-4-chloroquinoline 
• 26759-46-6 methyl 2-amino-4,5-dimethoxybenzoate 
• 13794-72-4 3H-6,7-dimethoxyquinazolin-4-one 

Downstream Products

• 475108-60-2 N-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-phenyl}-N'-(4,5-dimethyl-1,3-thiazol-2-yl)urea 
• 475108-31-7 N-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-phenyl}-N'-(3-methyl-5-isothiazolyl)urea 
• 475108-25-9 N-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-phenyl}-N'-(3-methyl-5-isoxazolyl)urea 
• 475108-24-8 N-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-phenyl}-N'-(5-methyl-3-isoxazolyl)urea 
• 475108-59-9 N-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-phenyl}-N'-(4-methyl-1,3-thiazol-2-yl)urea 
• 475108-58-8 N-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-phenyl}-N'-(5-methyl-1,3-thiazol-2-yl)urea 
• 475108-57-7 N-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-phenyl}-N'-(1,3-thiazol-2-yl)urea 
• 286370-17-0 N-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-phenyl}-N'-propylurea 

Relevant academic research and scientific papers

Quinazoline compound and application thereof

The invention relates to a quinazoline-containing compound as shown in a general formula (I), and a pharmaceutically acceptable salt, a solvate and a prodrug thereof, wherein substituent groups R1, R2, R3, R4, R5, R6, p, m and n are defined in the specification. The invention also relates to application of the compound shown in the general formula (I) in preparation of antitumor drugs, and also relates to application of the compound, the pharmaceutically acceptable salt, the solvate and the prodrug thereof in preparation and/or prevention and alleviation of cancers caused by tumor cells of human tissues or organs, wherein the cancers are preferably colon cancer, liver cancer, lymphoma, lung cancer, esophageal cancer, breast cancer, central nervous system tumor, melanoma, skin cancer, ovarian cancer, cervical cancer, kidney cancer, leukemia, prostate cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, nasopharyngeal cancer or gastric cancer and the like.

Structure–activity relationship study of novel quinazoline-based 1,6-naphthyridinones as MET inhibitors with potent antitumor efficacy

As a privileged scaffold, the quinazoline ring is widely used in the development of EGFR inhibitors, while few quinazoline-based MET inhibitors are reported. In our ongoing efforts to develop new MET-targeted anticancer drug candidates, a series of quinaz

Multi-target kinase inhibitor, pharmaceutical composition and preparation method and application of multi-target kinase inhibitor

The invention belongs to the technical field of biological medicines, in particular relates to a multi-target kinase inhibitor and a pharmaceutical composition containing the multi-target kinase inhibitor, and also relates to a preparation method and appl

PHENOXYQUINAZOLINE COMPOUNDS AND THEIR USE IN TREATING CANCER

The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 have any of the meanings hereinbefore defined in the description; process for their prepar

Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors

While the treatment of gastrointestinal stromal tumors (GISTs) has been revolutionized by the application of targeted tyrosine kinase inhibitors capable of inhibiting KIT-driven proliferation, diverse mutations to this kinase drive resistance to establish

URACIL DERIVATIVES AS AXL AND C-MET KINASE INHIBITORS

The present invention provides compounds of Formula I, or pharmaceutically acceptable salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c,Y, R3, X, E and G are as defined herein, methods of treatment and uses thereof.

Synthesis and structure-activity relationships of (aryloxy)quinazoline ureas as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors

In our continuing search for medicinal agents to treat proliferative diseases, quinazoline derivatives were synthesized and evaluated pharmacologically as epithelial growth factor receptor and vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase inhibitors. A quantitative structure-activity relationship analysis was conducted to rationalize the structure-activity relationship and to predict how similar the inhibitor-binding profiles of two protein kinases are likely to be on the basis of the docking of lead coumpounds into the ATP-binding site. This model was used to direct the synthesis of new compounds. A series of N-(aromatic)-N′-{4-[(6,7- dimethoxyquinazolin-4-yl)oxy]phenyl}urea were identified as potent and selective inhibitors of the tyrosine kinase activity of VEGFR-2 (fetal liver kinase 1, kinase insert domain-containing receptor). An efficient route was developed that enabled the synthesis of a wide variety of analogues with substitution on several positions of the template. Substitution of diarylurea, competitive with ATP, afforded several analogues with low nanomolar inhibition of enzymatic activity of VEGFR-2. In this paper, we describe the synthesis, structure-activity relationships, and pharmacological characterization of the series.

Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases

A new series of Quinazoline Ether Inhibitor which potently inhibits VEGFR-2 and PDGFR tyrosine kinases is described here. In vitro, pharmacokinetics and in vivo evaluations led to the selection of AZD2932.

Impact of aryloxy-linked quinazolines: A novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors

Three series of 6,7-dimethoxyquinazoline derivatives substituted in the 4-position by aniline, N-methylaniline and aryloxy entities, targeting EGFR and VEGFR-2 tyrosine kinases, were designed and synthesized. Pharmacological activities of these compounds

Design, synthesis, and DNA-binding of N-alkyl(anilino)quinazoline derivatives

New N-alkylanilinoquinazoline derivatives 5, 12, 20, and 22 have been prepared from 4-chloro-6,7-dimethoxyquinazoline 3, 4-chloro-6,7- methylenedioxyquinazoline 19, and commercially available anilines. Differents classes of compounds substituted by an aryloxygroup (6a-c, 16a,b, and 17a,b), (aminophenyl)ureas (12a,b and 13a-f), anilines (4a-m, 20a,b), N-alkyl(aniline) (5a-m, 21a,b, 22a,d), and N-aminoalkyl(aniline) (22e-g) have been synthesized. These molecules were evaluated for their cytotoxic activities and as potential DNA intercalating agents. We studied the strength and mode of binding to DNA of these molecules by DNA melting temperature measurements, fluorescence emission, and circular dichroism. The results of various spectral and gel electrophoresis techniques obtained with the different compounds, in particular compounds 5g and 22f, revealed significant DNA interaction. These experiments confirm that the N-aminoalkyl(anilino)-6,7-dimethoxyquinazoline nucleus is an efficient pharmacophore to trigger binding to DNA, via an intercalative binding process.