1379600-85-7

Upstream product

• 1379600-88-0 (Z)-ethyl 2-hydroxy-4-oxo-4-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)but-2-enoate 
• 142557-76-4 4-acetyl-4'-trifluoromethylbiphenyl 
• 99-90-1 para-bromoacetophenone 
• 128796-39-4 4-trifluoromethylphenylboronic acid 
• 636-99-7 4-nitrophenylhydrazine hydrochloride 

Downstream Products

• 1379600-87-9 1-(4-aminophenyl)-N-ethyl-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazole-3-carboxamide 
• 1333146-10-3 1-(4-(3-aminopropanamido)phenyl)-N-methyl-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazole-3-carboxamide 
• 1333146-12-5 1-(4-(3-aminopropanamido)phenyl)-N-ethyl-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazole-3-carboxamide 
• 1333146-14-7 1-(4-(3-aminopropanamido)phenyl)-N-isopropyl-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazole-3-carboxamide 
• 1333146-22-7 N-ethyl-1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazole-3-carboxamide 
• 1379600-86-8 N-ethyl-1-(4-nitrophenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazole-3-carboxamide 

Relevant academic research and scientific papers

INTEGRIN-LINKED KINASE INHIBITORS

A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula (I) or a pharmaceutically acceptable salt thereof are de

Identification and characterization of a novel integrin-linked kinase inhibitor

Integrin-linked kinase (ILK) represents a relevant target for cancer therapy in light of its role in promoting oncogenesis and tumor progression. Through the screening of an in-house focused compound library, we identified N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4′-(trifluoromethyl)-[1, 1′-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide (22) as a novel ILK inhibitor (IC50, 0.6 μM), which exhibited high in vitro potency against a panel of prostate and breast cancer cell lines (IC50, 1-2.5 μM), while normal epithelial cells were unaffected. Compound 22 facilitated the dephosphorylation of Akt at Ser-473 and other ILK targets, including glycogen synthase kinase-3β and myosin light chain. Moreover, 22 suppressed the expression of the transcription/translation factor YB-1 and its targets HER2 and EGFR in PC-3 cells, which could be rescued by the stable expression of constitutively active ILK. Evidence indicates that 22 induced autophagy and apoptosis, both of which were integral to its antiproliferative activity. Together, this broad spectrum of mechanisms underlies the therapeutic potential of 22 in cancer treatment, which is manifested by its in vivo efficacy as a single oral agent in suppressing PC-3 xenograft tumor growth.