41377-11-1

Upstream product

• 122-00-9 para-methylacetophenone 
• 1761-61-1 5-bromosalicyclaldehyde 

Downstream Products

• 1398523-25-5 C₁₈H₁₇BrN₂O₂ 
• 489441-32-9 C₁₆H₁₅BrN₂O 
• 1435462-14-8 1-(5-(5-bromo-2-(2,6-dinitro-4-(trifluoromethyl)-phenoxy)phenyl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone 
• 1537909-63-9 C₂₃H₁₆BrF₃N₄O₅ 
• 1537909-50-4 C₂₃H₁₄BrF₃N₂O₆ 

Relevant academic research and scientific papers

Synthesis and antimicrobial activity of some 5-chloro-3-phenyl-1H-indole-2-carbonyl azide derivatives

In the present investigations, a series of new 6-substituted-3-(5-chloro-3-phenyl-lJ?-indole-2yl)-3,4-dihydro-4-substituted-4-substituted-phenacyl-2H-l,3-benzoxazin-2-one 7a-f have been synthesized by two methods making use of 5-chloro-3-phenyl-l/H-ndole-2-carbonyl azide 2 and chalcones 5a-f. In one method, compound 2 on reaction with chalcones 5a-f in presence of triethylamine in dry benzene yields respective open chain carbamates 6a-f, followed by reaction with catalytic amount of potassium hydroxide in dry benzene under reflux condition to afford compounds 7a-f. In another method, compound 5a-f on reaction with compound 2 using dry benzene in presence of catalytic amount of potassium hydroxide under reflux conditions afford cyclized products 7a-f in good yield. Structures of the all the newly synthesized compounds have been confirmed by spectral data. All these compounds have been screened for their antibacterial activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, antifungal activity against Aspergillus Niger and Candida albicans and antituberculosis activity against Mycobacterium tuberculosis (H37RV).

Exploitation of new chalcones and 4H-chromenes as agents for cancer treatment

Chalcone and chromene derivatives were synthesized in good yield through simple and effective reactions using innocuous solvents such as water and ethanol and high yielding aldol condensations. Generally, the reactions were performed at room temperature, leading to the isolation of highly pure compounds. These compounds were tested on breast cancer cells (MCF-7 and Hs578T) and breast non-neoplastic cells (MCF-10A). After determination of IC50 value, specific assays were performed to analyze the potential of these compounds, and those bearing halogenated substituents presented enhanced activity comparing to methoxyl or methyl groups. More specifically, the bromine atom was often present in the bioactive molecules that proceeded to the final assays and showed to be promising candidates for further studies. The selected chromene acted as a cell migration inhibitory agent and triggered regulated cell death associated with G2/M cell-arrest and microtubule destabilization. For chalcones, the results suggest an anti-proliferative activity. Also, results for combination-therapy potentiated the antitumor effect of doxorubicin and reduced cytotoxicity in MCF-10A cells.

Synthesis, and antibacterial activity of novel 4,5-dihydro-1H-pyrazole derivatives as DNA gyrase inhibitors

A series of novel 4,5-dihydropyrazole derivatives (4a-4t), containing the dinitrobenzotrifluoride moiety, as DNA gyrase inhibitors were designed and synthesized. Based on the preliminary results, compounds 4d, 4h and 4t with potent inhibitory activity in

Synthesis, biological evaluation of novel 4,5-dihydro-2H-pyrazole 2-hydroxyphenyl derivatives as BRAF inhibitors

A series of novel 4,5-dihydropyrazole derivatives (3a-3t) containing hydroxyphenyl moiety as potential V600E mutant BRAF kinase (BRAF V600E) inhibitors were designed and synthesized. Docking simulation was performed to insert compounds 3d (1-(5-(5-chloro-2-hydroxyphenyl)-3-(p- tolyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone) and 3m (1-(3-(4-chlorophenyl)-5-(3, 5-dibromo-2-hydroxyphenyl)-4,5-dihydro-1H-pyrazol-1-yl)ethanone) into the crystal structure of BRAFV600E to determine the probable binding model, respectively. Based on the preliminary results, compound 3d and 3m with potent inhibitory activity in tumor growth may be a potential anticancer agent. Results of the bioassays against BRAFV600E, MCF-7 human breast cancer cell line and WM266.4 human melanoma cell line all showed several compounds had potent activities IC50 value in low micromolar range, among them, compound 3d and compound 3m showed strong potent anticancer activity, which were proved by that 3d: IC50 = 1.31 μM for MCF-7 and IC50 = 0.45 μM for WM266.5, IC50 = 0.22 μM for BRAFV600E, 3m: IC50 = 0.97 μM for MCF-7 and IC50 = 0.72 μM for WM266.5, IC50 = 0.46 μM for BRAFV600E, which were comparable with the positive control Erlotinib.

Hepatocyte growth factor pathway activators in chronic obstructive pulmonary disease

Methods are provided for treating chronic obstructive pulmonary diseases such as emphysema using compounds that activate the signaling pathways of hepatocyte growth factor.