878375-93-0

Upstream product

• 385785-16-0 (E/Z)-N'-(2-cyano-5-hydroxy-4-methoxyphenyl)-N,N-dimethyl-formimidamide 
• 107-04-0 1-Bromo-2-chloroethane 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 

Downstream Products

• 723282-92-6 N-(3-fluorophenyl)-2-(2-(7-(2-chloroethoxy)-6-methoxyquinazolin-4-yl-amino)-1,3-thiazol-5-yl)acetamide 

Relevant academic research and scientific papers

Quinazoline-1-deoxynojirimycin hybrids as high active dual inhibitors of EGFR and α-glucosidase

A series of novel quinazoline-1-deoxynojirimycin hybrids were designed, synthesized and evaluated for their inhibitory activities against two drug target enzymes, epidermal growth factor receptor (EGFR) tyrosine kinase and α-glucosidase. Some synthesized compounds exhibited significantly inhibitory activities against the tested enzymes. Comparing with reference compounds gefitinib and lapatinib, compounds 7d, 8d, 9b and 9d showed higher inhibitory activities against EGFR (IC50: 1.79–10.71 nM). Meanwhile the inhibitory activities of 7d, 8d and 9c against α-glucosidase (IC50 = 0.14, 0.09 and 0.25 μM, respectively) were obvious higher than that of miglitol (IC50 = 2.43 μM), a clinical using α-glucosidase inhibitor. Interestingly, compound 9d as a dual inhibitor showed high inhibitory activity to EGFRwt tyrosine kinase (IC50 = 1.79 nM), also to α-glucosidase (IC50 = 0.39 μM). The work could be very useful starting point for developing a new series of enzyme inhibitors targeting EGFR and/or α-glucosidase.

QUINAZOLINE COMPOUNDS

Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a sulphur atom and optionally containing one or more nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.