26196-58-7

Upstream product

• 2741-55-1 N-(4-(2-nitrophenoxy)phenyl)acetamide 
• 91804-89-6 4-(2-nitro-phenoxy)-phenyl isocyanate 
• 103-90-2 4-acetaminophenol 
• 123-30-8 4-amino-phenol 
• 1493-27-2 ortho-nitrofluorobenzene 
• 92017-56-6 4-(2-nitro-phenoxy)-benzoyl azide 
• 91692-79-4 4-(2-nitro-phenoxy)-benzoyl chloride 
• 577-19-5 2-nitrophenyl bromide 

Downstream Products

• 1381761-39-2 C₃₀H₃₅N₉O₇ 
• 1381761-41-6 C₂₇H₃₃N₉O₅ 
• 1381761-40-5 C₃₀H₃₇N₉O₅ 
• 76838-59-0 1-Benzoyl-3-[2-(4-dimethylamino-phenoxy)-phenyl]-thiourea 
• 76841-41-3 2-[2-(4-Dimethylamino-phenoxy)-phenylimino]-imidazolidine 
• 76839-40-2 [2-(4-Dimethylamino-phenoxy)-phenyl]-thiourea 
• 76847-82-0 C₁₄H₁₆N₂O 
• 104272-67-5 2-(4-dimethylaminophenoxy)-1-nitrobenzene 

Relevant academic research and scientific papers

Structure-Based Optimization of 3-Phenyl-N-(2-(3-phenylureido)ethyl)thiophene-2-sulfonamide Derivatives as Selective Mcl-1 Inhibitors

Selective Mcl-1 inhibitors may overcome the drug resistance caused by current anti-apoptotic Bcl-2 protein inhibitors in tumors with Mcl-1 overexpression. Based on previously discovered compounds with a 3-phenylthiophene-2-sulfonamide core moiety, in this work, we have obtained new compounds with improved binding affinity and/or selectivity under the guidance of structure-based design. The most potent compounds achieved sub-micromolar binding affinities to Mcl-1 (Ki～ 0.4 μM) and good cytotoxicity (IC5015N-heteronuclear single-quantum coherence NMR spectra suggested that these compounds bound to the BH3-binding groove on Mcl-1. Several cellular assays revealed that FWJ-D4 as well as its precursor FWJ-D5 effectively induced caspase-dependent apoptosis, and their target engagement at Mcl-1 was confirmed by co-immunoprecipitation experiments. Treatment with FWJ-D5 at 50 mg/kg every 2 days on an RS4;11 xenograft mouse model for 22 days led to 75% reduction in tumor volume without body weight loss.

MODULATORS OF HISTONE METHYLTRANSFERASE, AND METHODS OF USE THEREOF

Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.

ISOXAZOLINE, ISOTHIAZOLINE AND PYRAZOLINE FACTOR XA INHIBITORS

Isoxazolines, isothiazolines and pyrazolines which are inhibitors of Factor Xa, pharmaceutical compositions containing these compounds, and methods of using these compounds as anticoagulant agents for treatment and prevention of thromboembolic disorders. The compounds can be represented by the formula: STR1 where X is O, S or NR 15.