1262888-20-9

Basic information

• Product Name: N-(4-chlorobenzyl)-6-fluoroquinazoline-4-amine
• Synonyms: N-(4-chlorobenzyl)-6-fluoroquinazoline-4-amine
• CAS NO: 1262888-20-9
• Molecular Weight: 287.724
• Mol File: 1262888-20-9.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: N-(4-chlorobenzyl)-6-fluoroquinazoline-4-amine(CAS DataBase Reference)
• NIST Chemistry Reference: N-(4-chlorobenzyl)-6-fluoroquinazoline-4-amine(1262888-20-9)
• EPA Substance Registry System: N-(4-chlorobenzyl)-6-fluoroquinazoline-4-amine(1262888-20-9)

Safety Data

• Hazardous Substances Data: 1262888-20-9(Hazardous Substances Data)

Upstream product

• 16499-56-2 6-fluoro-3,4-dihydroquinazolin-4-one 
• 63069-49-8 2-amino-5-fluorobenzamide 
• 16499-56-2 6-fluoroquinazolin-4-ol 
• 446-08-2 2-amino-5-fluorobenzoic acid 
• 104-86-9 4-chlorobenzylamine 
• 16499-61-9 4-chloro-6-fluoro-quinazoline 

Relevant articles and documents

Synthesis, modelling, and anticonvulsant studies of new quinazolines showing three highly active compounds with low toxicity and high affinity to the GABA-A receptor

Some novel fluorinated quinazolines (5a-j) were designed and synthesized to be evaluated for their anticonvulsant activity and their neurotoxicity. Structures of all newly synthesized compounds were confirmed by their infrared (IR), mass spectrometry (MS) spectra, 1H nuclear magnetic resonance (NMR), 13C-NMR, and elemental analysis (CHN). The anticonvulsant activity was evaluated by a subcutaneous pentylenetetrazole (scPTZ) test and maximal electroshock (MES)-induced seizure test, while neurotoxicity was evaluated by a rotorod test. The molecular docking was performed for all newly-synthesized compounds to assess their binding affinities to the GABA-A receptor in order to rationalize their anticonvulsant activities in a qualitative way. The data obtained from the molecular modeling was correlated with that obtained from the biological screening. These data showed considerable anticonvulsant activity for all newly-synthesized compounds. Compounds 5b, 5c, and 5d showed the highest binding affinities toward the GABA-A receptor, along with the highest anticonvulsant activities in experimental mice. These compounds also showed low neurotoxicity and low toxicity in the median lethal dose test compared to the reference drugs. A GABA enzymatic assay was performed for these highly active compounds to confirm the obtained results and explain the possible mechanism for anticonvulsant action. The most active compounds might be used as leads for future modification and optimization.

POTENT SMALL MOLECULE INHIBITORS OF AUTOPHAGY, AND METHODS OF USE THEREOF

Certain aspects of the invention relates to small molecule autophagy inhibitors, and their use for treatment and prevention of cancers and acute pancreatitis. As disclosed herein, a small molecule inhibitor of autophagy was been identified from an image-based screen in a known bioactive library. It was found that this autophagy inhibitor functions by promoting the degradation of type III PI3 kinase complex which is required for initiating autophagy. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity.