39147-10-9

Upstream product

• 1122-17-4 dichloromaleic acid anhydride 
• 98-16-8 3-trifluoromethylaniline 

Downstream Products

• 143947-28-8 2-Thioxo-6-(3-trifluoromethyl-phenyl)-[1,3]dithiolo[5,6][1,4]dithiino[2,3-c]pyrrole-5,7-dione 
• 143947-33-5 6-(3-Trifluoromethyl-phenyl)-[1,3]dithiolo[5,6][1,4]dithiino[2,3-c]pyrrole-2,5,7-trione 
• 1073612-93-7 4-[[2,5-dioxo-1-[3-(trifluoromethyl)phenyl]-3-pyrrolidinyl]thio]benzoic acid 
• 451487-04-0 C₁₈H₁₀ClF₃N₂O₄ 
• 415701-55-2 C₁₅H₁₂ClF₃N₂O₃ 
• 369398-74-3 C₁₆H₁₅ClF₃N₃O₂ 
• 451487-05-1 C₁₇H₁₇ClF₃N₃O₂ 
• 958727-71-4 C₁₇H₁₇ClF₃N₃O₃ 
• 958735-05-2 C₁₉H₂₁ClF₃N₃O₄ 
• 452369-11-8 C₂₁H₁₇ClF₃N₃O₂ 
• 804535-13-5 C₂₂H₁₉ClF₃N₃O₂ 
• 958729-41-4 C₁₉H₁₅ClF₃N₅O₂ 
• 958729-40-3 C₂₂H₁₉ClF₃N₃O₃ 
• 958728-49-9 C₁₆H₁₅ClF₃N₃O₂ 

Relevant academic research and scientific papers

Inhibition of Bfl-1 with N-aryl maleimides

High-throughput screening of 66,000 compounds using competitive binding of peptides comprising the BH3 domain to anti-apoptotic Bfl-1 led to the identification of 14 validated 'hits' as inhibitors of Bfl-1. N-Aryl maleimide 1 was among the validated 'hits'. A chemical library encompassing over 280 analogs of 1 was prepared following a two-step synthesis. Structure-activity studies for inhibition of Bfl-1 by analogs of N-aryl maleimide 1 revealed a preference for electron-withdrawing substituents in the N-aryl ring and hydrophilic amines appended to the maleimide core. Inhibitors of Bfl-1 are potential development candidates for anti-cancer therapeutics.

Thiazolidinone CFTR inhibitors with improved water solubility identified by structure-activity analysis

The thiazolidinone 3-[(3-trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone (CFTRinh-172) inhibits cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel conductance with submicromolar affinity and blocks cholera toxin-induced intestinal fluid secretion. Fifty-eight CFTRinh-172 analogs were synthesized to identify CFTR inhibitors with improved water solubility, exploring modifications in its two phenyl rings, thiazolidinone core, and core-phenyl connectors. Greatest CFTR inhibition potency was found for 3-CF3 and polar group-substituted-phenyl rings, and a thiazolidinone core. Two compounds with ～1 μM CFTR inhibition potency and solubility >180 μM (>10-fold more than CFTRinh-172) were identified: Tetrazolo-172, containing 4-tetrazolophenyl in place of 4-carboxyphenyl, and Oxo-172, containing thiazolidinedione in place of the thiazolidinone core. These water soluble thiazolidinone analogs had low cellular toxicity. The improved water solubility of Tetrazolo- and Oxo-172 make them potential lead candidates for therapy of secretory diarrheas and polycystic kidney disease.