52791-04-5

Upstream product

• 290-87-9 1,3,5-Triazine 
• 99358-09-5 7-amino-2,3-dihydrobenzo[b][1,4]dioxine-6-carboxylic acid 
• 1207868-16-3 7,8-dihydro[1,4]dioxino[2,3-g]quinazoline 
• 22013-33-8 6-amino-3,4-benzodioxane 
• 20197-76-6 7-amino-2,3-dihydro-benzo[1,4]dioxine-6-carboxylic acid methyl ester 

Downstream Products

• 52791-05-6 4-chloro-7,8-dihydro[1,4]-dioxino[2,3-g]quinazoline 
• 1456819-61-6 (7,8-dihydro[1,4]dioxino[2,3-g]quinazolin-4-yl)-(3'-methansulfonamidopheyl)amine hydrochloride 
• 1401243-69-3 (7,8-dihydro[1,4]dioxino[2,3-g]quinazolin-4-yl)-(biphenyl-3'-yl)amine hydrochloride 

Relevant academic research and scientific papers

1,4-Dioxane-fused 4-anilinoquinazoline as inhibitors of epidermal growth factor receptor kinase

The 4-anilinoquinazoline PD 153035 (1) is a potential antitumor agent which acts by inhibiting tyrosine kinase activity of epidermal growth factor receptor (EFGR) via competitive binding at the ATP site of enzyme. A series of cyclic analogues of PD 153035 bearing the 1,4-dioxane ring was prepared by reaction of 6-chloro derivative 5 with several aniline nucleophiles. These were evaluated for their ability to inhibit the EGFR kinase and the growth of primary human tumor cell cultures. All of the new 4-anilinoquinazolines exhibited less potency than PD 153035 against EGFR kinase. However, compounds 2b, 2c, 2e, 2g, and 2h showed higher inhibitory activities than PD 153035 against the growth of A431 tumor cell line. The compound 2b containing 3-chloroaniline ring was as potent as PD 153035 against EGFR kinase and showed about 5.4-fold better potency than PD1 53035 in the inhibition of growth of A431 cell line with good selectivity.

Substituted quinazolinones as kinase inhibitors endowed with anti-fibrotic properties

Some new 3-substituted quinazolinones were synthesized and evaluated as inhibitors of kinases involved in fibrogenic process. The compounds were tested against a panel of both tyrosine and serine-threonine kinases. The profile of selectivity of some representative compounds was investigated through molecular docking studies. The most interesting compounds were also evaluated in vitro as potential agents for the treatment of fibrotic diseases. Quinazolinone derivatives reduced proliferation and expression of genes involved in the fibrogenic process in hepatic stellate cells (HSCs) and intestinal subepithelial myofibroblasts (ISEMFs). Furthermore some compounds downregulated phosphorylation of p38MAPK. Our findings provide evidences that 3-substituted quinazolinones target multiple essential pathways of the fibrogenic process.

Quinazoline-based multi-tyrosine kinase inhibitors: Synthesis, modeling, antitumor and antiangiogenic properties

In this work the synthesis and the biological evaluation of some novel anilinoquinazoline derivatives carrying modifications in the quinazoline scaffold and in the aniline moiety were reported. Preliminary cytotoxicity studies identified three derivatives

Exploring Epidermal Growth Factor Receptor (EGFR) inhibitor features: The role of fused dioxygenated rings on the quinazoline scaffold

A number of dioxolane, dioxane, and dioxepine quinazoline derivatives have been synthetized, and evaluated as EGFR inhibitors. Their cytotoxic activity has been tested against two cell, lines overexpressing and not expressing EGFR. Most derivatives were a

QUINAZOLINE DERIVATIVES AS RAF KINASE MODULATORS AND METHODS OF USE THEREOF

Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.

Bi-4-[1-(quinazolinyl-4)piperidyls] and bis{4-[1-(quinazolinyl-4)piperidyl]alkanes}

Disclosed are bi-4-[1-(quinazolinyl-4)piperidyls] and bis{4-[1-(quinazolinyl-4)piperidyl]alkanes}, e.g. 1,3-bis{4-[1-(6,7-dimethylquinazolinyl-4)piperidyl]propane}, having pharmacological activity in animals and useful for example, as anti-obesity and anti-diabetic agents. Said compounds may be prepared by reacting a 4-haloquinazoline with bi-4-piperidyl or a bis(piperidyl-4)alkane.

N,N-Bis(4-Quinazolinyl)alkanediamines

Disclosed are N,N'-Bis(4-Quinazolinyl)alkanediamines, e.g., N,N'-Bis(7-chloro-4-quinazolinyl)-1,9-nonanediamine, having pharmacological activity in animals and useful for example, as anti-obesity agents. Said compounds may be prepared by reacting a 4-haloquinazoline with an alkanediamine.