1334602-74-2

Upstream product

• 16499-57-3 7-fluoro-3,4-dihydroquinazolin-4-one 
• 151504-81-3 methyl 4-fluoro-2-nitrobenzoate 
• 404010-84-0 methyl 2-amino-4-morpholinobenzoate 
• 16499-57-3 7-fluoro-3H-quinazolin-4-one 
• 446-32-2 4-fluoroanthranilic acid 
• 404010-74-8 2-amino-4-(morpholin-4-yl)benzoic acid 
• 1265848-98-3 7-morpholin-4-yl-3H-quinazolin-4-one 
• 1334602-76-4 4-(4-methoxybenzyloxy)-7-morpholin-4-yl-quinazoline 
• 1334602-75-3 7-bromo-4-((4-methoxybenzyl)oxy)quinazoline 
• 573675-55-5 7-bromo-4-chloro-quinazoline 
• 194851-16-6 7-bromoquinazolin-4(3H)-one 
• 20776-50-5 2-amino-4-bromobenzoic acid 

Relevant academic research and scientific papers

Aryl quinazoline DNA-PK inhibitor

The invention belongs to the technical field of medicines, and particularly relates to aryl quinazoline DNA-PK inhibitor compounds, pharmaceutically acceptable salts and isomers thereof, pharmaceutical compositions and preparations containing the compounds, the pharmaceutically acceptable salts and the isomers thereof, methods for preparing the compounds, the pharmaceutically acceptable salts andthe stereoisomers thereof, and uses of the compounds, pharmaceutically acceptable salts thereof, and isomers thereof.

Design, synthesis and biological evaluation of pyrazolylaminoquinazoline derivatives as highly potent pan-fibroblast growth factor receptor inhibitors

Fibroblast growth factor receptors (FGFRs) are important oncology targets due to the dysregulation of this signaling pathway in a wide variety of human cancers. We identified a series of pyrazolylaminoquinazoline derivatives as potent FGFR inhibitors with low nanomolar potency. The representative compound 29 strongly inhibited FGFR1-3 kinase activity and suppressed FGFR signaling transduction in FGFR-addicted cancer cells; FGFRs-driven cell proliferation was also strongly inhibited regardless of mechanistic complexity implicated in FGFR activation, which further confirmed that 29 was a potent pan-FGFR inhibitor. The flexibility of our structure offered the potential to preserve good affinity for mutant FGFR, which is important for developing TKIs with long-term efficacy.

Morpholinylquinazolines

The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in claim 1, and/or physiologically acceptable salts, tautomers and stereo-isomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.