1086063-46-8

Usage

Uses

Used in Pharmaceutical Industry:
N-(5-bromo-2-methoxypyridin-3-yl)-2,4-difluorobenzenesulfonamide is used as a building block for the synthesis of heterocyclic compounds, which are important in the development of new drugs. Its unique structure and potential biological activity make it a promising candidate for pharmaceutical applications.
Used in Agrochemical Industry:
N-(5-bromo-2-methoxypyridin-3-yl)-2,4-difluorobenzenesulfonamide is used as a chemical intermediate in the synthesis of agrochemicals. Its potential biological activity and unique structure contribute to the development of new agrochemical products.
Used in Organic Synthesis:
N-(5-bromo-2-methoxypyridin-3-yl)-2,4-difluorobenzenesulfonamide is used as a chemical intermediate in organic synthesis. Its presence in the synthesis of various heterocyclic compounds makes it a valuable component in the creation of complex organic molecules.

Upstream product

• 884495-39-0 5-bromo-2-(methyloxy)-3-pyridinamine 
• 13918-92-8 2,4-difluorobenzene-1-sulfonyl chloride 
• 67443-38-3 5-bromo-2-chloro-3-nitropyridine 
• 15862-34-7 5-bromo-3-nitro-2-pyridone 
• 152684-30-5 5-bromo-2-methoxy-3-nitropyridine 

Downstream Products

• 1135310-10-9 2,4-difluoro-N-(2-methoxy-5-(4-(4-morpholinyl)pyrido[3,2-d]pyrimidin-6-yl)-3-pyridinyl)benzenesulfonamide 
• 1086062-66-9 GS⁽²⁶⁴⁾K₂₁₅₈ 
• 1360537-73-0 2,4-difluoro-N-(2-hydroxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide 

Relevant academic research and scientific papers

Development of anti-breast cancer PI3K inhibitors based on 7-azaindole derivatives through scaffold hopping: Design, synthesis and in vitro biological evaluation

Breast cancer is the cancer with the highest incidence all over the world. Phosphatidylinositol 3-kinase is an important regulator of intracellular signaling pathways, which is frequently mutated and overexpressed in majority of human breast cancers, and the inhibition of PI3K has been considered as a promising approach for the treatment of the cancer. Here, we report our design and synthesis of new 7-azaindole derivatives as PI3K inhibitors through the scaffold hopping strategy. By varying the groups at the 3-position of 7-azaindole, we identified a series of potent PI3K inhibitors, whose antiproliferative activities against two human breast cancer MCF-7 and MDA-MB-231 cell lines were evaluated. Representative derivatives FD2054 and FD2078 showed better activity than BKM120 in antiproliferation, reduced the levels of phospho-AKT and induced cell apoptosis. All these results suggested that FD2054 and FD2078 are potent PI3K inhibitors that could be considered as potential candidates for the development of anticancer agents.

PI3 KINASE INHIBITORS AND USES THEREOF

A compound of the formula (II); a pharmaceutical composition comprising same; and methods for treating a fibrotic disease in a subject.

PI3K/mTOR protein degradation targeting chimeric compound as well as preparation method and medical application of PI3K/mTOR protein degradation targeting chimeric compound

The invention relates to a PI3K/mTOR protein degradation targeting chimeric body (PROTAC) compound as well as a preparation method and medical application thereof. Specifically, the present inventionrelates to a compound represented by a general formula (

Imidazopyrazine derivative and synthesis method and application thereof

The invention discloses 6-(6 substituent group-5-sulfonamido-3-pyridine) imidazo [1, 2-a] pyrazine derivatives as shown in a formula (I) or pharmaceutically acceptable salts thereof. The invention also discloses application of the 6-(6-substituent-5-sulfo

FIBROBLAST ACTIVATION PROTEIN (FAP) TARGETED IMAGING AND THERAPY IN FIBROSIS

Excessive deposition of extracellular matrix is a hallmark of Idiopathic pulmonary fibrosis (IPF), it is advantageous to target the cells and the mechanisms associated with this process. By targeting myofibroblasts (specialized contractile fibroblasts) th

Identification of novel thiazolo[5,4-b]pyridine derivatives as potent phosphoinositide 3-kinase inhibitors

A series of novel 2-pyridyl, 4-morpholinyl substituted thiazolo[5,4-b]pyridine analogues have been designed and synthesized in this paper. These thiazolo[5,4-b]pyridines were efficiently prepared in seven steps from commercially available substances in mo

Design, synthesis, and biological evaluation of some novel 4-aminoquinazolines as Pan-PI3K inhibitors

A series of 4-aminoquinazolines derivatives containing hydrophilic group were designed and identified as potent Pan-PI3K inhibitors in this study. The results of antiproliferative assays in vitro showed that this series of compounds had strong inhibition of tumor growth, especially compound 7b for MCF-7 cells but weak inhibition to normal cells. PI3K kinase assay showed that 7b had high activity for three PI3K isoforms with the IC50 values of picomole. The western blot assay indicated that 7b could decrease the phospho-Akt (S473) in a dose-dependent manner. Further experiments showed that 7b could induce apoptosis in MCF-7 cells. Four key hydrogen bonding interactions were found in the docking of 7b with PI3K kinase. All these results suggested that 7b is a potent PI3K inhibitor and could be considered as a potential candidate for the development of anticancer agents.

Aromatic heterocyclic compound serving as PI3K/mTOR kinase regulator and preparation method and application of aromatic heterocyclic compound

The invention discloses 6-(6-substituted group-5-sulfonamido-3-pyridinyl)imidazo[1,2-a]pyridines shown as a formula (I) or 6-(6-substituted group-5-sulfonamido-3-pyridinyl)imidazo[1,2-b]pyridazine derivatives or pharmaceutically acceptable salts thereof and a preparation method. The invention also discloses application of 6-(6-substituted group-5-sulfonamido-3-pyridinyl)imidazo[1,2-a]pyridines or6-(6-substituted group-5-sulfonamido-3-pyridinyl)imidazo[1,2-b]pyridazine derivatives or pharmaceutically acceptable salts thereof to preparation of medicines for resisting tumors, treating cerebral ischemia and treating diabetes mellitus as a PI3K/mTOR inhibitor.

Design, synthesis and evaluation of some 1,6-disubstituted-1H-benzo[d]imidazoles derivatives targeted PI3K as anticancer agents

Phosphatidylinositol 3-kinase (PI3K) pathway regulates various cellular processes, such as proliferation, growth, autophagy and apoptosis. Class I PI3K is frequently mutated and overexpressed in a lot of human cancers and PI3K was considered as a target for therapeutic treatment of cancer. In this study, we designed and synthesized a series of 1,6-disubstituted-1H-benzo[d]imidazoles derivatives and evaluated their anticancer activity and the compound 8i was identified as a lead compound. Compound 8i with the most potent antiproliferative activity was selected for further biological mechanism. The PI3K kinase assay have shown potent efficiency against four subtypes of PI3K with an IC50 of 0.5–1.9 nM. Molecular docking showed a possible formation of H-bonding with essential amino acid residues. Meanwhile, western blot assay indicated that 8i inhibited cell proliferation via suppression of PI3K kinase activity and subsequently blocked PI3K/Akt pathway activation in HCT116 cells. In addition, 8i could inhibit the migration and invasion ability of HCT116 cells and could induce apoptosis of HCT116 cells.

Micro-reactor tandem synthesis method of indole anticancer drug molecules

The invention relates to a micro-reactor tandem synthesis method of indole anticancer drug molecules. The method comprises the following steps: a reaction liquid 1 and a reaction liquid 2 are mixed, then are introduced into a first micro-reactor, and are reacted to obtain a first effluent, the first effluent and a reaction liquid 3 are mixed, then are introduced into a second micro-reactor, and are reacted to obtain a second effluent, the second effluent and a reaction liquid 4 are mixed, then are introduced into a third micro-reactor, and are reacted to obtain a final effluent, and the finaleffluent is concentrated and separated to obtain the indole anticancer drug molecules, wherein the reaction liquid 1 is a mixed solution containing 5-bromine-3-amino-2-substituted (R1)-pyridine, the reaction liquid 2 is substituted (R2)-benzenesulfonyl chloride, the reaction liquid 3 is a mixed solution containing bis(pinacolato)diboron, the reaction liquid 4 is a mixed solution containing a 5-bromo-7-azaindole derivative, and the indole anticancer drug molecules are benzenesulfonamidopyridylazaindole compounds. Compared with the prior art, the method of the invention has the advantages of high reaction efficiency, few side reactions and simple production process.