547739-67-3

Upstream product

• 2548-29-0 3-(chlorosulfonyl)-4-methylbenzoic acid 
• 99-75-2 4-methyl-benzoic acid methyl ester 
• 99-94-5 p-Toluic acid 

Downstream Products

• 651728-83-5 3-chlorosulfonyl-4-methylbenzoic acid 2-(p-tolylsulfonyl)ethyl ester 

Relevant academic research and scientific papers

Synthesis, 3D-structure and stability analyses of NRPa-308, a new promising anti-cancer agent

We report herein the synthesis of a newly described anti-cancer agent, NRPa-308. This compound antagonizes Neuropilin-1, a multi-partners transmembrane receptor overexpressed in numerous tumors, and thereby validated as promising target in oncology. The p

Discovery and in Vitro Optimization of 3-Sulfamoylbenzamides as ROMK Inhibitors

Inhibitors of the renal outer medullary potassium channel (ROMK) show promise as novel mechanism diuretics, with potentially lower risk of diuretic-induced hypokalemia relative to current thiazide and loop diuretics. Here, we report the identification of a novel series of 3-sulfamoylbenzamide ROMK inhibitors. Starting from HTS hit 4, this series was optimized to provide ROMK inhibitors with good in vitro potencies and well-balanced ADME profiles. In contrast to previously reported small-molecule ROMK inhibitors, members of this series were demonstrated to be highly selective for inhibition of human over rat ROMK and to be insensitive to the N171D pore mutation that abolishes inhibitory activity of previously reported ROMK inhibitors.

Identification and Optimization of Anthranilic Acid Based Inhibitors of Replication Protein A

Replication protein A (RPA) is an essential single-stranded DNA (ssDNA)-binding protein that initiates the DNA damage response pathway through protein-protein interactions (PPIs) mediated by its 70N domain. The identification and use of chemical probes that can specifically disrupt these interactions is important for validating RPA as a cancer target. A high-throughput screen (HTS) to identify new chemical entities was conducted, and 90 hit compounds were identified. From these initial hits, an anthranilic acid based series was optimized by using a structure-guided iterative medicinal chemistry approach to yield a cell-penetrant compound that binds to RPA70N with an affinity of 812 nm. This compound, 2-(3- (N-(3,4-dichlorophenyl)sulfamoyl)-4-methylbenzamido)benzoic acid (20 c), is capable of inhibiting PPIs mediated by this domain.

Inhibitors of Neuropilin and use thereof for the treatment of Neuropilin-related diseases

The present invention relates to a compound of general formula (I), and salts or solvate thereof, for treating a Neuropilin-related disease, disorder or condition; and to a composition, a pharmaceutical composition and a medicament comprising the compound of general formula (I).

INHIBITOR OF NEUROPILIN AND USE THEREOF FOR THE TREATMENT OF NEUROPILIN-RELATED DISEASES

The present invention relates to a compound of general formula (I), and salts or solvate thereof, for treating a Neuropilin-related disease, disorder or condition; and to a composition, a pharmaceutical composition and a medicament comprising the compound of general formula (I).

1-arylsulfonyl-2-(Pyridylmethylsulfinyl) benzimidazoles as new proton pump inhibitor prodrugs

New arylsulfonyl proton pump inhibitor (PPI) prodrug forms were synthesized. These prodrugs provided longer residence time of an effective PPI plasma concentration, resulting in better gastric acid inhibition.