914919-18-9

Upstream product

• 1194-02-1 4-fluorobenzonitrile 
• 99-10-5 3,5-Dihydroxybenzoic acid 
• 1256592-07-0 ethyl 3,5-bis(4-cyanophenoxy)benzoate 
• 4142-98-7 ethyl 3,5-dihydroxybenzoate 

Downstream Products

• 914919-19-0 4,4′-((5-carboxy-1,3-phenylene)bis(oxy))dibenzoic acid 
• 1611481-98-1 C₃₂H₃₁N₃O₆ 
• 1256590-54-1 4,4'-((5-(naphthalene-2-sulfonamido)-1,3-phenylene)bis(oxy))dibenzimidamide 
• 1256590-55-2 4,4'-((5-(4-fluorophenylsulfonamido)-1,3-phenylene)bis(oxy))dibenzimidamide 
• 1256590-65-4 N-(3,5-bis(4-carbamimidoylphenoxy)phenyl)-1-(2-hydroxyethyl)piperidine-4-carboxamide 
• 1256590-59-6 (1r,4r)-4-amino-N-(3,5-bis(4-carbamimidoylphenoxy)phenyl)cyclohexanecarboxamide 
• 1256590-61-0 1-(2-aminoethyl)-N-(3,5-bis(4-carbamimidoylphenoxy)phenyl)piperidine-4-carboxamide 
• 1256590-63-2 1-(3-aminopropanoyl)-N-(3,5-bis(4-carbamimidoylphenoxy)phenyl)piperidine-4-carboxamide 
• 1611482-05-3 (1r,4r)-4-aminocyclohexyl 3,5-bis(4-carbamimidoylphenoxy)benzoate 
• 1611481-73-2 3,5-bis(4-carbamimidoylphenoxy)-N-(4-fluorophenyl)benzamide 
• 1256589-45-3 4,4'-((5-(1,2,3,4-tetrahydroisoquinoline-2-carbonyl)-1,3-phenylene)bis(oxy))dibenzimidamide 
• 1256589-39-5 4,4'-((5-(decahydroquinoline-1-carbonyl)-1,3-phenylene)bis(oxy))dibenzimidamide 
• 1256590-26-7 1-(3,5-bis(4-carbamimidoylphenoxy)benzoyl)piperidine-4-carboxylic acid 
• 1256590-87-0 ethyl 4-(3,5-bis(4-carbamimidoylphenoxy)benzamido)piperidine-1-carboxylate 

Relevant academic research and scientific papers

Structure-guided discovery of 1,3,5 tri-substituted benzenes as potent and selective matriptase inhibitors exhibiting in vivo antitumor efficacy

Matriptase is a serine protease implicated in cancer invasion and metastasis. Expression of matriptase is frequently dysregulated in human cancers and matriptase has been reported to activate latent growth factors such as hepatocyte growth factor/scatter factor, and proteases such as urokinase plasminogen activator suggesting that matriptase inhibitors could have therapeutic potential in treatment of cancer. Here we report a structure-based approach which led to the discovery of selective and potent matriptase inhibitors with benzene as central core having 1,3,5 tri-substitution pattern. X-ray crystallography of one of the potent analogs in complex with matriptase revealed strong hydrogen bonding and salt-bridge interactions in the S1 pocket, as well as strong CH-π contacts between the P2/P4 cyclohexyl and Trp215 side-chain. An additional interaction of the pendant amine at cyclohexyl with Gln175 side-chain results in substantial improvement in matriptase inhibition and selectivity against other related serine proteases. Compounds 15 and 26 showed tumor growth inhibition in a subcutaneous DU-145 prostate cancer mouse model. These compounds could be useful as tools to further explore the biology of matriptase as a drug target.

A porous metal-organic framework based on Zn6O2 clusters: Chemical stability, gas adsorption properties and solvatochromic behavior

A highly connected 3D metal-organic framework with tfz-d topology based on Zn6O2 clusters and flexible carboxylate ligands has been synthesized. The obtained Zn-MOF shows solvatochromic behavior for fluorescence sensing of small molecules, gas adsorption properties and exceptional chemical stability and might have applications for separation and detection purposes.

PROTEASE INHIBITORS

A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility