578737-95-8

Basic information

• Product Name: 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-6-iodo-
• CAS NO: 578737-95-8
• Molecular Formula: C14H8ClFIN3
• Molecular Weight: 399.594
• Mol File: 578737-95-8.mol
• Article Data: 10

Chemical Properties

• CAS DataBase Reference: 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-6-iodo-(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-6-iodo-(578737-95-8)
• EPA Substance Registry System: 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-6-iodo-(578737-95-8)

Safety Data

• Hazardous Substances Data: 578737-95-8(Hazardous Substances Data)

Upstream product

• 903597-10-4 N’-(2-cyano-4-iodophenyl)-N,N-dimethyl formamidine 
• 367-21-5 3-chloro-4-fluorophenylamine 
• 1885-29-6 anthranilic acid nitrile 
• 132131-24-9 5-iodoanthranilonitrile 
• 98556-31-1 4-chloro-6-iodoquinazoline 
• 77317-55-6 methyl 2-amino-5-iodobenzoate 
• 16064-08-7 6-iodo-4-hydroxyquinazoline 

Downstream Products

• 1421356-86-6 N-(3-chloro-4-fluorophenyl)-6-(5-formyl-2-furyl)-4-quinazolinamine 
• 1421356-78-6 N-(3-chloro-4-fluorophenyl)-6-(5-(((2-(cyclohexenyl)ethyl)amino)methyl)-2-furyl)-4-quinazolinamine 
• 1421356-77-5 N-(3-chloro-4-fluorophenyl)-6-(5-(((2-(4-nitrophenyl)ethyl)amino)methyl)-2-furyl)-4-quinazolinamine 
• 1421356-73-1 N-(3-chloro-4-fluorophenyl)-6-(5-(((propyl)amino)methyl)-2-furyl)-4-quinazolinamine 
• 659747-32-7 (3-chloro-4-fluoro-phenyl)-[6-(1-ethoxy-vinyl)-quinazolin-4-yl]-amine 
• 659747-53-2 N-{4-[4-(3-chloro-4-fluoro-phenylamino)-quinazolin-6-yl]-thiazol-2-ylmethyl}-2,2,2-trifluoro-N-(2-methanesulfonyl-ethyl)-acetamide 

Relevant articles and documents

Novel 4-arylaminoquinazolines bearing N,N-diethyl(aminoethyl)amino moiety with antitumour activity as EGFRwt-TK inhibitor

Herein, four novel 4-arylaminoquinazoline derivatives with N,N-diethyl(aminoethyl)amino moiety were designed, synthesised and evaluated on biological activities in vitro. All synthesised compounds have inhibitory effects against tumour cells (SW480, A549, A431 and NCI-H1975). In particular, 4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)-6-(5-((N,N-diethyl(aminoethyl))aminomethyl)furan-2-yl)quinazoline (6a) and 6-(5-((N,N-diethylethyl)aminomethyl)furan-2-yl)-4-(4-(E)-(propen-1-yl)phenylamino)quinazoline (6d) were potent antitumour agents which showed high antiproliferative activities against tumour cells in vitro. Moreover, compound 6a could induce late apoptosis of A549 cells at high concentrations and arrest cell cycle of A549 cells in the G0/G1 phase at tested concentrations. Also, compound 6a could inhibit the activity of wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) with IC50 value of 15.60 nM. Molecular docking showed that compound 6a formed three hydrogen bonds with EGFRwt-TK, while lapatinib formed only two hydrogen bonds with the receptor protein. It is believed that this work would be giving a reference for developing anti-cancer drugs targeted EGFR-TK.

Compounds capable of inhibiting ErbB/HDAC and preparation method thereof, and pharmaceutical composition comprising compounds and application thereof

The invention relates to compounds capable of inhibiting ErbB/HDAC and a preparation method thereof, and a pharmaceutical composition comprising the compounds and application thereof. The compounds are disclosed as Formula 1. The compounds or pharmaceutically acceptable salts, solvates, esters, acids, metabolites or prodrugs thereof, or the pharmaceutical composition comprising the compounds can be used for preparing ErbB kinases and HDAC activity inhibitors and also preparing ErbB-kinase/HDAC-activated mediated disease curatives.

Novel compound having tumor diagnosis or tumor growth inhibitory activity on EGFR mutant and medical uses comprising the same

The present invention relates to a novel compound having activities of diagnosing a tumor having an epidermal growth factor receptor (EGFR) mutant and inhibiting tumor growth, a salt thereof, a contrast medium comprising the same, and a pharmaceutical composition for treating or preventing EGFR-related cancer diseases comprising the same as an active ingredient. The novel compound or the salt thereof according to the present invention does not inhibit a wild type EGFR but selectively inhibits an EGFR variant, and thus can treat and prevent EGFR-related cancer diseases, including lung cancer, colon cancer or breast cancer. Particularly, the compound or the salt thereof according to the present invention can effectively treat and prevent non-small cell lung cancer upon which Iressa or Tarceva cannot have any significant effect. In addition, the compound or the salt thereof according to the present invention responses with a target of Gefitinib-sensitive cancer cells or cancer cells showing EGFR T790M mutation rather than wild type EGFR over-expressed cancer cells, and thus can be used advisably as a contrast medium capable of clearly differentiating EGFR-related cancer cells by imaging.COPYRIGHT KIPO 2017