210755-57-0

Upstream product

• 459-46-1 4-Fluorobenzyl bromide 
• 825-90-1 sodium p-hydroxybenzenesulfonate 
• 637-89-8 4-sulfanylphenol 
• 15015-57-3 bis(4-hydroxyphenyl)disulfide 
• 10580-19-5 4-hydroxybenzenesulfonic acid sodium salt dihydrate 
• 625814-06-4 bis[4-(4-fluorobenzyloxy)phenyl]disulfide 

Downstream Products

• 259132-81-5 (2R,3S)-2-[4-(4-Fluoro-benzyloxy)-benzenesulfonylamino]-3-hydroxy-butyric acid methyl ester 
• 211381-44-1 2R,3S-1-[4-(4-fluorobenzyloxy)-benzenesulfonyl]-3-isopropoxycarbonylamino-piperidine-2-carboxylic acid 
• 683210-05-1 4-(4-Fluoro-benzyloxy)-N-[(1R,2S)-2-hydroxy-1-(4-methyl-2,6,7-trioxa-bicyclo[2.2.2]oct-1-yl)-propyl]-benzenesulfonamide 
• 683204-95-7 (2R,3R)-1-[4-(4-Fluoro-benzyloxy)-benzenesulfonyl]-3-methyl-aziridine-2-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

Selective arylsulfonamide inhibitors of ADAM-17: Hit optimization and activity in ovarian cancer cell models

Activated leukocyte cell adhesion molecule (ALCAM) is expressed at the surface of epithelial ovarian cancer (EOC) cells and is released in a soluble form (sALCAM) by ADAM-17-mediated shedding. This process is relevant to EOC cell motility and invasiveness, which is reduced by inhibitors of ADAM-17. In addition, ADAM-17 plays a key role in EGFR signaling and thus may represent a useful target in anticancer therapy. Herein we report our hit optimization effort to identify potent and selective ADAM-17 inhibitors, starting with previously identified inhibitor 1. A new series of secondary sulfonamido-based hydroxamates was designed and synthesized. The biological activity of the newly synthesized compounds was tested in vitro on isolated enzymes and human EOC cell lines. The optimization process led to compound 21, which showed an IC 50 of 1.9 nM on ADAM-17 with greatly increased selectivity. This compound maintained good inhibitory properties on sALCAM shedding in several in vitro assays.

Efficient route for the preparation of benzyloxy-substituted benzenesulfonyl chlorides from mercaptophenols

A consistently high-yielding route has been developed for the preparation of benzyloxybenzenesulfonyl chlorides from mercaptophenols. This route allows rapid preparation of intermediates for array chemistry.

Arylsulfonyl hydroxamic acid derivatives

A compound of the formula wherein R1, R2R3, R4R5, R6, R7, R8, R9and Q are as defined above, useful in the treatment of a condition selected from the group c

DOPAMINE RECEPTOR MODULATORS AS ANTIPSYCHOTIC AGENTS

The invention provides compounds of formula (I):wherein A and B represent the groups -(CH2)m- and -(CH2)n-respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydroge