73035-17-3

Upstream product

• 17071-24-8 1-(3-amino-4-methylphenyl)ethanone 
• 5333-27-7 1-(4-methyl-3-nitro-phenyl)-ethanone 

Downstream Products

• 70958-70-2 5-acetyl-2-methylbenzenesulfonamide 
• 70958-71-3 5-((2-Bromo-1-oxo)ethyl)-2-methylbenzenesulfonamide 
• 87086-28-0 5-{1-Hydroxy-2-[2-(2-methoxyphenoxy)-1-methylethylamino]-ethyl}-2-methylbenzenesulfonamide 
• 345948-56-3 5-{2-[Benzyl-(1-methyl-2-phenoxy-ethyl)-amino]-1-hydroxy-ethyl}-2-methyl-benzenesulfonamide 
• 344751-99-1 5-{2-[Benzyl-(1-methyl-3-phenyl-propyl)-amino]-1-hydroxy-ethyl}-2-methoxy-benzenesulfonamide 
• 345948-57-4 5-{2-[Benzyl-(1-methyl-2-phenoxy-ethyl)-amino]-acetyl}-2-methyl-benzenesulfonamide 
• 344752-15-4 5-(2-{Benzyl-[2-(2-hydroxy-phenoxy)-1-methyl-ethyl]-amino}-1-hydroxy-ethyl)-2-methyl-benzenesulfonamide 
• 344754-82-1 5-(2-{Benzyl-[2-(4-methoxy-phenoxy)-1-methyl-ethyl]-amino}-1-hydroxy-ethyl)-2-methyl-benzenesulfonamide 
• 344755-07-3 5-(2-{Benzyl-[2-(3-methoxy-phenoxy)-1-methyl-ethyl]-amino}-1-hydroxy-ethyl)-2-methyl-benzenesulfonamide 
• 344754-90-1 5-(2-{Benzyl-[3-(2-methoxy-phenyl)-1-methyl-propyl]-amino}-1-hydroxy-ethyl)-2-methyl-benzenesulfonamide 
• 344752-02-9 5-{2-[Benzyl-(1-methyl-3-phenyl-propyl)-amino]-acetyl}-2-methoxy-benzenesulfonamide 
• 71140-59-5 5-(2-{Benzyl-[3-(2-methoxy-phenyl)-1-methyl-propyl]-amino}-acetyl)-2-methyl-benzenesulfonamide 
• 70958-81-5 5-(2-{Benzyl-[2-(2-methoxy-phenoxy)-1-methyl-ethyl]-amino}-1-hydroxy-ethyl)-2-methyl-benzenesulfonamide 
• 344752-20-1 5-(2-{Benzyl-[2-(2-hydroxy-phenoxy)-1-methyl-ethyl]-amino}-acetyl)-2-methyl-benzenesulfonamide 

Relevant academic research and scientific papers

Fragment-based drug discovery of 2-thiazolidinones as BRD4 inhibitors: 2. Structure-based optimization

The signal transduction of acetylated histone can be processed through a recognition module, bromodomain. Several inhibitors targeting BRD4, one of the bromodomain members, are in clinical trials as anticancer drugs. Hereby, we report our efforts on discovery and optimization of a new series of 2-thiazolidinones as BRD4 inhibitors along our previous study. In this work, guided by crystal structure analysis, we reversed the sulfonamide group and identified a new binding mode. A structure-activity relationship study on this new series led to several potent BRD4 inhibitors with IC50 of about 0.05-0.1 μM in FP binding assay and GI50 of 0.1-0.3 μM in cell based assays. To complete the lead-like assessment of this series, we further checked its effects on BRD4 downstream protein c-Myc, investigated its selectivity among five different bromodomain proteins, as well as the metabolic stability test, and reinforced the utility of 2-thiazolidinone scaffold as BET bromodomain inhibitors in novel anticancer drug development.

Process for preparing N,N-dialkylaniline salt of 5-acetyl-2-alkylbenzene sulfonic acid

Process for preparing 2-alkyl-5-haloacetylbenzenesulfonamide represented by the general formula (1), STR1 (wherein R1 is an alkyl group having 1 to 5 carbon atoms; and X is a chlorine atom, bromine atom or iodine atom), characterized by halogen