873306-25-3

Upstream product

• 64-18-6 formic acid 
• 10428-49-6 β-chloro-β-nitrostyrene 
• 72982-21-9 2-amino-4-phenylfuran-3-carbonitrile 
• 582-24-1 1-phenyl-2-hydroxyethanone 
• 141764-36-5 5-phenylfuro<2,3-d>pyrimidin-4(3H)-one 

Downstream Products

• 943230-38-4 6-[(5-Phenylfuro[2,3-d]pyrimidin-4-yl)amino]hexanoic acid methyl ester 
• 1208346-65-9 6-bromo-4-chloro-5-phenylfuro[2,3-d]pyrimidine 
• 1208346-51-3 2-(5-phenylfuro[2,3-d]pyrimidin-4-ylamino)ethanol 
• 1321619-04-8 N-(3-fluoro-4-(5-phenylfuro[2,3-d]pyrimidin-4-yloxy)phenyl)-1-(4-fluoro phenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide 
• 1192754-00-9 1-phenyl-3-(4-{2-[(5-phenylfuro[2,3-d]pyrimidin-4-yl)-amino]ethyl}phenyl)urea 
• 1610549-26-2 C₁₇H₁₅N₅OS 
• 1610549-18-2 1-(3-chlorophenyl)-3-(5-(2-(5-phenylfuro[2,3-d]pyrimidin-4-ylamino)ethyl)thiazol-2-yl)urea 
• 1301608-94-5 1-(4-(5-phenylfuro[2,3-d]pyrimidin-6-yl)phenyl)cyclobutanamine 
• 1301610-83-2 tert-butyl (1-(4-(5-phenylfuro[2,3-d]pyrimidin-6-yl)phenyl)cyclobutyl)carbamate 
• 1301610-82-1 6-iodo-5-phenylfuro[2,3-d]pyrimidine 
• 1301610-81-0 5-phenylfuro[2,3-d]pyrimidine 

Relevant academic research and scientific papers

PHARMACEUTICAL COMPOSITION AND APPLICATION REPLACING QUINOLONE DERIVATIVE, PHARMACEUTICAL ACCEPTABLE SALT, OR STEREOISOMER

Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.

4-Oxo-1,4-dihydroquinoline-3-carboxamide Derivatives as New Axl Kinase Inhibitors

Axl is a new potential target for anticancer drug discovery. A series of 4-oxo-1,4-dihydroquinoline-3-carboxamides were designed and synthesized as highly potent Axl kinase inhibitors. One of the most promising compounds, 9im, tightly bound with Axl prote

Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine aurora kinase inhibitor

Ligand efficiency (LE) and lipophilic efficiency (LipE) are two important indicators of "drug-likeness", which are dependent on the molecule's activity and physicochemical properties. We recently reported a furano-pyrimidine Aurora kinase inhibitor 4 (LE = 0.25; LipE = 1.75), with potent activity in vitro; however, 4 was inactive in vivo. On the basis of insights obtained from the X-ray co-crystal structure of the lead 4, various solubilizing functional groups were introduced to optimize both the activity and physicochemical properties. Emphasis was placed on identifying potential leads with improved activity as well as better LE and LipE by exercising tight control over the molecular weight and lipophilicity of the molecules. Rational optimization has led to the identification of Aurora kinase inhibitor 27 (IBPR001; LE = 0.26; LipE = 4.78), with improved in vitro potency and physicochemical properties, resulting in an in vivo active (HCT-116 colon cancer xenograft mouse model) anticancer agent.

Novel, Cyclically Substituted Furopyrimidine Derivatives and Use Thereof

The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.

Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d] pyrimidine or furo[2,3-d]pyrimidine scaffold

A series of thieno[2,3-d]pyrimidines and furo[2,3-d]pyrimidines were synthesized and evaluated for the c-Met inhibition. Thieno[2,3-d]pyrimidine 6b stood out as the most potent showing an IC50 of 35.7 nM. This compound displayed high inhibitory effect on cell proliferation in BaF3-TPR-Met cells and showed high selectivity for c-Met family against other 14 tested kinases. However, compound 6b was found ineffective in the c-Met-dependent U-87MG human gliobastoma xenograft model that may be relevant to its poor PK profile.

Identification, SAR studies, and X-ray Co-crystallographic analysis of a novel furanopyrimidine aurora kinase a inhibitor

Herein we reveal a simple method for the identification of novel Aurora kinase A inhibitors through substructure searching of an in-house compound library to select compounds for testing. A hydrazone fragment conferring Aurora kinase activity and heterocy

Novel, Acyclically Substituted Furopyrimidine Derivatives and Use Thereof

The present application relates to novel, acyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.

FURANOPYRIMIDINES

The present invention relates to furanopyrimidine compounds having the general Formula (I) and stereoisomers, tautomers, solvates, pharmaceutically acceptable salts and derivatives, and prodrugs thereof. The invention also includes pharmaceutical compositions comprising a compound of Formula (I), methods of treating various diseases and conditions in a mammal, including inflammation, inhibition of T cell activation, proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma and thymoma, comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I). The invention also relates to methods of manufacturing medicaments, which comprise one or more compounds of Formula (I).