157671-99-3

Upstream product

• 50413-24-6 2-bromo-1-(4-methanesulfonylphenyl)ethanone 
• 405-50-5 p-Fluorophenylacetic acid 
• 100-68-5 methyl-phenyl-thioether 
• 98-86-2 acetophenone 
• 21382-98-9 p-cyanophenyl methyl sulfide 
• 10297-73-1 4-(methanesulfonyl)acetophenone 
• 1778-09-2 4-(Methylthio)acetophenone 

Downstream Products

• 157672-00-9 3-(4-fluorophenyl)-4-<4-(methylsulfonyl)phenyl>-5H-furan-2-one 
• 168299-81-8 1-<2-(4-fluorophenyl)-4,4-bis(hydroxymethyl)cyclopenten-1-yl>-4-(methylsulfonl)benzene 
• 159429-83-1 1-<2-(4-fluorophenyl)-4,4-dicarbomethoxycyclopenten-1-yl>-4-(methylsulfonyl)benzene 
• 168299-84-1 1-<2-(4-fluorophenyl)-4,4-bis(tosylmethyl)cyclopenten-1-yl>-4-(methylsulfonyl)benzene 
• 168433-84-9 SC-58451 
• 168299-83-0 4-[6-(4-fluorophenyl)spiro[2.4]hept-5-en-5-yl]benzenesulfonamide 
• 179174-91-5 2-(4-fluorophenyl)-3-<4-(methylsulfonyl)phenyl>-1,4-dihydroxy-2-butene 

Relevant academic research and scientific papers

Stereoselective synthesis and anti-proliferative effects on prostate cancer evaluation of 5-substituted-3,4-diphenylfuran-2-ones

Series of 5-substituted-3,4-diphenylfuran-2-ones were stereoselectively prepared. Their potential anti-proliferative effects on prostate cancer and some of their cyclooxygenases (COXs) inhibitory activities were evaluated. Structure-activity relationship (SAR) data, acquired by substituent modification at the para-position and ortho-position of the C-3 phenyl ring and 5-substituted modification of the central furanone, showed that 3-(2-chloro-phenyl)-4-(4-methanesulfonyl-phenyl)-5-(1-methoxy-ethyl) -5H-furan-2-one (13p) was the most potent compound and could effectively reduce the proliferation of prostate cancer cells (PC3 cell IC50 = 20 μM; PC3 PCDNA cell IC50 = 5 μM; PC3 SKP2 cell IC50 = 5 μM; DU145 cell IC50 = 25 μM). The cell cycle analysis for 13p in DU145 indicated that 13p may induce G1 phase arrest.

Pyridyl substituted spirodienes for the treatment of inflammation

A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: STR1 wherein A is selected from STR2 wherein each of R1 through R10 is independently selected from hydrido, halo, alkyl, alkoxy, alkylthio, cyano, haloalkyl, haloalkoxy, hydroxyalkyl; alkoxyalkyl, hydroxyl, mercapto, alkylsulfonyl, haloalkylsulfonyl, and sulfamyl; and wherein n is a number selected from 0, 1, 2 and 3; or a pharmaceutically-acceptable salt thereof.

Method of preparing sulfmonamides from sulfones

A one-pot synthesis of sulfonamides from sulfones has been developed. Conversion of sulfones to the corresponding sulfinic acid salts is followed by oxidative-amination to give the sulfonamides.

Substituted cyclopentenes for the treatment of inflammation

A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: STR1 wherein each of R1 and R2 is independently selected from alkyl, hydrido, hydroxyalkyl, halo, haloalkyl, alkoxycarbonyl and carboxyl; wherein R5 is selected from alkylsulfonyl, haloalkylsulfonyl and sulfamyl; and wherein B is phenyl or pyridyl, wherein B is optionally substituted at a substitutable position with alkyl, halo, alkylthio, cyano, haloalkyl, alkoxy, hydroxyalkyl and alkoxyalkyl; or a pharmaceutically-acceptable salt thereof.

Diarylspiro[2.4]heptenes as orally active, highly selective cyclooxygenase-2 inhibitors: Synthesis and structure-activity relationships

A novel series of 5,6-diarylspiro[2.4]hept-5-enes was shown to provide highly potent and selective cyclooxygenase-2 (COX-2) inhibitors. A study of structure-activity relationships in this series suggests that 3,4- disubstituted phenyl analogs are generally more selective than 4-substituted phenyl analogs and that replacement of the methyl sulfone group on the 6- phenyl ring with a sulfonamide moiety results in compounds with superior in vivo pharmacological properties, although with lower COX-2 selectivity. Several compounds have been shown to possess promising pharmacological properties in adjuvant-induced arthritis and edema analgesia models. The absence of gastrointestinal (GI) toxicity at 200 mpk of several selected compounds in rats and mice corresponds well with the weak potency for inhibition of COX-1 observed in the enzyme assay. Methyl sulfone 55 and sulfonamide 24 were shown to have superior in vivo pharmacological profiles, low GI toxicity, and good oral bioavailability and duration of action.

Substituted spiro compounds for the treatment of inflammation

A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: STR1 wherein n is a number selected from 0, 1 and 2; wherein R3 is methylsulfonyl or sulfamyl; and wherein R8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.