891785-30-1

Usage

Uses

Used in Pharmaceutical Industry:
6-Bromo-3-fluoroisoquinoline is used as a key intermediate for the synthesis of various biologically active molecules and materials. Its unique structure and properties make it a valuable building block in the development of new drugs and therapeutic agents.
Used in Medicinal Chemistry:
6-Bromo-3-fluoroisoquinoline is employed as a versatile compound in medicinal chemistry, contributing to the discovery and design of novel drug candidates with potential applications in treating various diseases and conditions.
Used in Drug Discovery:
6-Bromo-3-fluoroisoquinoline is utilized as a starting point for drug discovery, enabling researchers to explore its potential in the development of new pharmaceuticals with improved efficacy and safety profiles.
Used in Antimicrobial Applications:
6-Bromo-3-fluoroisoquinoline is used as an antimicrobial agent, demonstrating effectiveness against a range of microorganisms, which can contribute to the development of new antibiotics and antifungal agents.
Used in Antitumor Applications:
6-Bromo-3-fluoroisoquinoline is used as an antitumor agent, showing promise in the treatment of cancer due to its ability to target and inhibit the growth of tumor cells.

Upstream product

• 891785-28-7 6-bromo-isoquinolin-3-ylamine 
• 934343-53-0 benzyl-(6-bromo-isoquinolin-3-yl)-amine 
• 552331-06-3 6-bromo-3-chloro-isoquinoline 

Downstream Products

• 1105710-34-6 3-fluoroisoquinolin-6-ylboronic acid 
• 1574396-46-5 6-bromo-N-(1,3-dimethyl-1H-pyrazol-5-yl)-isoquinolin-3-amine 

Relevant academic research and scientific papers

Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3)

PRMT3 catalyzes the asymmetric dimethylation of arginine residues of various proteins. It is crucial for maturation of ribosomes and has been implicated in several diseases. We recently disclosed a highly potent, selective, and cell-active allosteric inhibitor of PRMT3, compound 4. Here, we report comprehensive structure-activity relationship studies that target the allosteric binding site of PRMT3. We conducted design, synthesis, and evaluation of novel compounds in biochemical, selectivity, and cellular assays that culminated in the discovery of 4 and other highly potent (IC50 values: ～10-36 nM), selective, and cell-active allosteric inhibitors of PRMT3 (compounds 29, 30, 36, and 37). In addition, we generated compounds that are very close analogs of these potent inhibitors but displayed drastically reduced potency as negative controls (compounds 49-51). These inhibitors and negative controls are valuable chemical tools for the biomedical community to further investigate biological functions and disease associations of PRMT3.

SERINE/THREONINE KINASE INHIBITORS

Compounds having the formula I wherein R2, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE

The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

THIADIAZOLE MODULATORS OF PKB

The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the th

HETEROCYCLIC MODULATORS OF PKB

The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity

The structure-activity relationships of a series of isoquinoline-pyridine-based protein kinase B/Akt antagonists have been investigated in an effort to improve the major short-comings of the lead compound 3, including poor pharmacokinetic profiles in several species (e.g., mouse iv t1/2 = 0.3 h, po F = 0%). Chlorination at C-1 position of the isoquinoline improved its pharmacokinetic property in mice (iv t1/2 = 5.0 h, po F = 51%) but resulted in >500-fold drop in potency. In a mouse MiaPaCa-2 xenograft model, an amino analog 10y significantly slowed the tumor growth, however was accompanied by toxicity.