51310-29-3Relevant articles and documents
Discovery of 1,1′-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors
La Regina, Giuseppe,Coluccia, Antonio,Famiglini, Valeria,Pelliccia, Sveva,Monti, Ludovica,Vullo, Daniela,Nuti, Elisa,Alterio, Vincenzo,De Simone, Giuseppina,Monti, Simona Maria,Pan, Peiwen,Parkkila, Seppo,Supuran, Claudiu T.,Rossello, Armando,Silvestri, Romano
, p. 8564 - 8572 (2015/11/24)
New 1,1′-biphenylsulfonamides were synthesized and evaluated as inhibitors of the ubiquitous human carbonic anhydrase isoforms I, II, IX, XII, and XIV using acetazolamide (AAZ) as reference compound. The sulfonamides 1-21 inhibited all the isoforms, with Ki values in the nanomolar range of concentration, and were superior to AAZ against all of them. X-ray crystallography and molecular modeling studies on the adducts that compound 20, the most potent hCA XIV inhibitor of the series (Ki = 0.26 nM), formed with the five hCAs, provided insight into the molecular determinants responsible for the high affinity of this molecule toward the target enzymes. The results pave the way to the development of 1.1′-biphenylsulfonamides as a new class of highy potent hCA XIV inhibitors.
Synthesis of unsymmetrical biaryl ketones via palladium-catalyzed carbonylative cross-coupling reaction of arylboronic acids with iodoarenes
Ishiyama,Kizaki,Miyaura,Suzuki
, p. 7595 - 7598 (2007/10/02)
The cross-coupling reaction between arylboronic acids, carbon monoxide (1 atm), and aryl iodides in the presence of palladium catalyst and base provided unsymmetrical biaryl ketones in high yields. The choice of a suitable base and solvent was essential to achieve selective formation of the unsymmetrical biaryl ketone without a biaryl by-product.
