129112-65-8

Usage

Uses

Used in Pharmaceutical Industry:
2,4-dichloro-7-nitroquinazoline is used as a key intermediate for the synthesis of 4-phenoxy-2-(1-piperazinyl)quinazolines. These quinazoline derivatives exhibit potent anticonvulsive and antihypoxic properties, making them valuable in the treatment of seizures and hypoxic conditions. The compound's ability to form these therapeutic agents highlights its importance in the development of new medications for neurological disorders.
Additionally, 2,4-dichloro-7-nitroquinazoline is used to prepare quinazoline-based stem cell mobilizers that target the chemokine receptor CXCR4. These mobilizers play a crucial role in the field of regenerative medicine, as they can potentially enhance the migration and homing of stem cells to damaged tissues, promoting tissue repair and regeneration.

Upstream product

• 619-17-0 4-Nitroanthranilic acid 
• 951-97-3 2-acetamido-4-nitrobenzoic acid 
• 2879-79-0 N-(2-methyl-5-nitrophenyl)acetamide 
• 174565-63-0 7-nitro-1,2,3,4-tetrahydro-quinazoline-2,4-dione 

Downstream Products

• 129112-48-7 2-(4-Methyl-piperazin-1-yl)-7-nitro-4-phenoxy-quinazoline 
• 129112-50-1 2-(4-Methyl-piperazin-1-yl)-4-phenoxy-quinazolin-7-ylamine 
• 129112-52-3 7-Chloro-2-(4-methyl-piperazin-1-yl)-4-phenoxy-quinazoline 
• 76004-97-2 N²-(3,4-dichlorophenyl)-N⁴-<2-(diethylamino)ethyl>-7-nitro-2,4-quinazolinediamine 1.8-hydrochloride 
• 129112-64-7 2-Chloro-7-nitro-4(3H)-quinazolinone 

Relevant academic research and scientific papers

INHIBITORS OF CYCLIN-DEPENDENT KINASES

Provided herein are compounds which are inhibitors of cyclin-dependent kinases (CDKs), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.

Design, synthesis and biological evaluation of 2-aminoquinazolin-4(3H)-one derivatives as potential SARS-CoV-2 and MERS-CoV treatments

Despite the rising threat of fatal coronaviruses, there are no general proven effective antivirals to treat them. 2-Aminoquinazolin-4(3H)-one derivatives were newly designed, synthesized, and investigated to show the inhibitory effects on SARS-CoV-2 and MERS-CoV. Among the synthesized derivatives, 7-chloro-2-((3,5-dichlorophenyl)amino)quinazolin-4(3H)-one (9g) and 2-((3,5-dichlorophenyl)amino)-5-hydroxyquinazolin-4 (3H)-one (11e) showed the most potent anti-SARS-CoV-2 activities (IC50 50 50 > 25 μM). In addition, both compounds showed acceptable results in metabolic stabilities, hERG binding affinities, CYP inhibitions, and preliminary PK studies.

DIACYLGLYCEROL KINASE MODULATING COMPOUNDS

The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.

Discovery of 2-(2-aminopyrimidin-5-yl)-4-morpholino-N-(pyridin-3-yl)quinazolin-7-amines as novel PI3K/mTOR inhibitors and anticancer agents

In this study, a series of novel 7 or 8-substituted 4-morpholine-quinazoline derivatives was designed and synthesized. Their PI3Kα inhibitory activities, antiproliferative activities against seven cancer cell lines, namely, PC-3, DU145, MCF-7, BT474, SK-BR-3, U937 and A431, were evaluated in vitro. Compound 17f proved to be a potential drug candidate with high PI3Kα inhibition activity (IC50 = 4.2 nM) and good antiproliferative activity. Compound 17f was also tested for its inhibitory activities against other kinases, such as PI3Kβ, PI3Kγ, PI3Kδ and mTOR, its effects on p-Akt (S473) and cell cycle. These results suggested that compound 17f could significantly inhibit the PI3K/Akt/mTOR pathway as a potent PI3K inhibitor and anticancer agent.

Tricyclic dicarbonyl derivatives

Compounds of general formula (Ia), (Ib) and (II), wherein R1 and R2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R3 R4 NS(O)2 -- and R3 and R4 signify lower alkyl, and R2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH2 NHCH3, a bicyclic heterocycle with 1-3N atoms or a group --NR5 R6 or --OR5 in which R5 and R6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies --CH=CH--, --CH=N--, --NH--, --CO-- or --O--, as well as pharmaceutically usable salts of compounds of general formula (Ia), (Ib) and (II). They can be used for the treatment or prevention of illnesses, especially for the treatment or prevention of ischemia, hypoglycaemia, hypoxia, cerebral vascular spasms, spasticity, trauma, hemorrhagia, infection (viral, bacterial, amoebic, prional), epileptic seizures, autoimmune diseases, withdrawal symptoms, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, intoxications, olivoponto-cerebellar atrophy, spinal cord injuries, schizophrenia, depressions, anxiety states, dependence, pains,autism and mental retardation.