40889-42-7

Upstream product

• 108-24-7 acetic anhydride 
• 609-85-8 2-amino-3,5-dibromobenzoic acid 
• 118-92-3 anthranilic acid 
• 75-36-5 acetyl chloride 
• 81190-68-3 2-amino-4,6-dibromobenzoic acid 

Downstream Products

• 86993-60-4 N-[2,4-Dibromo-6-(morpholine-4-carbonyl)-phenyl]-acetamide 
• 130601-79-5 6,8-dibromo-3-p-methoxybenzylideneamino-2-methylquinazolin-4-one 
• 130601-78-4 2-acetamido-N-p-methoxybenzylideneamino-3,5-dibromobenzhydrazide 
• 78993-25-6 2-Acetylamino-3,5-dibromobenzoic acid hydrazide 
• 609-85-8 2-amino-3,5-dibromobenzoic acid 
• 88092-71-1 2-acetylamino-3,5-dibromophenyl ethyl ketone 
• 88092-72-2 6,8-dibromo-2,4,4,-trimethyl-3,1-benzoxazine 
• 88092-70-0 2-acetylamino-3,5-dibromo acetophenone 
• 76618-10-5 2-Methyl-3--6,8-dibromo-quinazolin(3H)-4-one 
• 88092-66-4 N-[2,4-Dibromo-6-(3,4-dimethyl-benzoyl)-phenyl]-acetamide 
• 88092-68-6 N-[2,4-Dibromo-6-(2,5-dimethyl-benzoyl)-phenyl]-acetamide 
• 130601-77-3 3-benzylideneamino-6,8-dibromo-2-styrylquinazolin-4-one 
• 77995-21-2 [4-(6,8-Dibromo-2-methyl-4-oxo-4H-quinazolin-3-yl)-phenylsulfanyl]-acetic acid 
• 78993-28-9 C₁₀H₁₀Br₂N₄O₃ 

Relevant academic research and scientific papers

Design, synthesis and evaluation of new quinazolin-4-one derivatives as apoptotic enhancers and autophagy inhibitors with potent antitumor activity

This work presents the design and synthesis of a series of new quinazolin-4-one derivatives, based on the established effectiveness of quinazoline-based small molecules as anticancer agents. Synthesized compounds were more potent against MCF-7 than A-549

Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases

Aberrant activation of FMS-like tyrosine receptor kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid leukemia (AML) in 20–30% of patients. In this study we identified a highly selective (phenylethenyl)quinazoline compound family as novel potent inhibitors of the FLT3-ITD and FLT3-D835Y kinases. Their prominent effects were confirmed by biochemical and cellular proliferation assays followed by mice xenograft studies. Our modelling experiments and the chemical structures of the compounds predict the possibility of covalent inhibition. The most effective compounds triggered apoptosis in FLT3-ITD AML cells but had either weak or no effect in FLT3-independent leukemic and non-leukemic cell lines. Our results strongly suggest that our compounds may become therapeutics in relapsing and refractory AML disease harboring various ITD and tyrosine kinase domain mutations, by their ability to overcome drug resistance.

Synthesis and bioactivities evaluation of novel vv-pyridylpyrazole derivatives with 1,2,3-triazole and quinazolin-4(3H)-one substructures

Two series of JV-pyridylpyrazole derivatives containing 1,2,3-triazole and quinazolin-4(3H)-one substructures were designed and synthesized. In total, 18 novel compounds were prepared, and all compounds were characterized by 1H NMR, 13C NMR and elemental

Synthesis, biological evaluation of 2,3-disubstituted-imidazolyl/benzimidazolyl-quinazolin-4(3H)-one derivatives

A series of disubstituted-quinazolin-4(3H)-ones derivatives have been synthesized and confirmed through IR, 1H- and 13C-NMR, MS spectroscopy and elemental analysis. Synthesized compounds were screened for in vitro and in vivo anti-inflammatory using human red blood cell membrane stabilization method and carrageenan-induced rat paw edema. The antimicrobial potency was measured by disk diffusion method. The compounds with imidazole (3g) and benzimidazole nucleus (4b and 4f) displayed a significant anti-inflammatory activity by in vitro method. Moreover, the compounds 3d and 4a exhibited a significant anti-inflammatory activity in vivo. The compounds 3d, 3f and 4g were found to be active antimicrobial agents, when compared with reference drug ciprofloxacin and amphotericin B. Thus, these compounds can serve as promising leads for further biological studies.

Dihydrofolate reductase inhibitors: Synthesis, characterization and biological evaluation of some novel 2,3-disubstituted quinazolinones

A series of some novel dihydrofolate reductase inhibitors (DHFR) of 2,3-disubstituted quinazolinone derivatives were synthesized by condensing benzoxazone derivatives with compounds containing primary amino group. The chemical structures of the newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, Mass spectral data and elemental analysis. The enzyme inhibitory activities were studied by using GLIDE 4.5 module. In vitro cytotoxic activity of the synthesized compounds was evaluated by MTT assay method. Compounds 3g and 5a exhibited good hydrogen bond interactions with the amino acid residue of DHFR and also showed significant cytotoxic activity.

Synthesis and anticonvulsant activity of novel quinazolin-4(3H)-one derived pyrazole analogs

Eighteen novel 6,8-(dibromo/unsubstituted)-2-(methyl/phenyl)-3-(4-(5- (substitutedphenyl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carbonyl)phenyl) -quinazolin-4(3H)-ones 4a-4r were designed and synthesized in good yield. Antiepileptic screening of the title compounds was performed using MES and scPTZ seizures tests while the neurotoxicity was determined by rotorod test. In the preliminary screening, compounds 4d, 4e, 4p, 4q, and 4r were found active in MES model, while 4a, 4d, 4f, 4m, and 4p showed significant antiepileptic activity in scPTZ model. Further, all these eight compounds were administered to rats and compounds 4e, 4p, and 4q showed better activity than Phenytoin in oral route. Among these compounds 4p revealed protection in MES after i.p. administration at a dose of 30 mg/kg (0.5 h) and 100 mg/kg (4 h). The compound 4p also provided protection in the scPTZ at a dose of 100 mg/kg (0.5 h) and 300 mg/kg (4 h).

Design, synthesis and anticonvulsant activities of novel 1-(substituted/unsubstituted benzylidene)-4-(4-(6,8-dibromo-2-(methyl/phenyl)-4- oxoquinazolin-3(4H)-yl)phenyl) semicarbazide derivatives

Novel quinazolinone derivatives 5a-5n were designed, synthesized and screened for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by rotorod test. Compounds 5c, 5d, 5g, 5j and 5k were found active in the prelim

Synthesis and evaluation of novel 2-substituted-quinazolin-4(3H)-ones as potent analgesic and anti-inflammatory agents

A novel series of 2-substituted-quinazolin-4(3H)-ones were synthesized by reacting 3,5-disubstituted-anthranilic acid with acetic anhydride/benzoyl chloride, which were further reacted with different primary amines to obtain 2,6,8-substituted-quinazolin-4(3H)-ones 6a-f, 7, 8. All the synthesized compounds were characterized and screened for analgesic and anti-inflammatory activities. Compounds 6,8-dibromo-2-phenyl-3-(4′-carboxyl phenyl)quinazolin-4(3H)-one 7 and 6,8-dibromo-2-phenyl-3-(2′- phenylethanoic acid)quinazolin-4(3H)-one 8 displayed good analgesic and anti-inflammatory activity in comparison to the reference standards acetyl salicylic acid and indomethacin, respectively.

Synthesis of some new substituted quinazolin-4-3H-ones as potent anticonvulsant agents

A new series of 3-(4-(2-(6,8-dibromo-3-(substituted phenyl)-4-oxo-3,4- dihydroquinazolin-2-y1)methyl) hydrazinyl)thiazol-2-y1)-2-phenylthiazolidin-4- ones were synthesized and their structures were elucidated on the basis of elemental analyses and spectro

Synthesis and antimicrobial activities of some novel substituted 2-imidazolyl-N-(4-oxo-quinazolin-3(4H)-yl)-acetamides

Several substituted-quinazolin-3(4H)-ones 8-11ad were synthesized by condensation of 2-chloro-N-(4-oxosubstituted-quinazolin-3(4H)-yl)-acetamides with various substituted imidazoles through one pot reaction. Elemental analysis, IR, 1H-NMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolin-4-one derivatives were investigated for their antitubercular, antibacterial and antifungal activities. Some of the tested compounds showed good antitubercular activity. None of the synthesized compounds showed significant antibacterial and antifungal activity.