174699-78-6Relevant articles and documents
Discovery of a 1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity
Wittman, Mark,Carboni, Joan,Attar, Ricardo,Balasubramanian, Balu,Balimane, Praveen,Brassil, Patrick,Beaulieu, Francis,Chang, Chiehying,Clarke, Wendy,Dell, Janet,Eummer, Jeffrey,Frennesson, David,Gottardis, Marco,Greer, Ann,Hansel, Steven,Hurlburt, Warren,Jacobson, Bruce,Krishnananthan, Subramaniam,Lee, Francis Y.,Li, Aixin,Lin, Tai-An,Liu, Peiying,Ouellet, Carl,Sang, Xiaopeng,Saulnier, Mark G.,Stoffan, Karen,Sun, Yax,Velaparthi, Upender,Wong, Henry,Yang, Zheng,Zimmermann, Kurt,Zoeckler, Mary,Vyas, Dolatrai
, p. 5639 - 5643 (2005)
Compound 3 (BMS-536924), a novel small-molecule inhibitor of the insulin-like growth factor receptor kinase with equal potency against the insulin receptor is described. The in vitro and in vivo biological activity of this interesting compound is also rep
Unmasking the Hidden Carbonyl Group Using Gold(I) Catalysts and Alcohol Dehydrogenases: Design of a Thermodynamically-Driven Cascade toward Optically Active Halohydrins
Escot, Lorena,González-Granda, Sergio,Gotor-Fernández, Vicente,Lavandera, Iván
, p. 2552 - 2560 (2022/02/16)
A concurrent cascade combining the use of a gold(I) N-heterocyclic carbene (NHC) and an alcohol dehydrogenase (ADH) is disclosed for the synthesis of highly valuable enantiopure halohydrins in an aqueous medium and under mild reaction conditions. The meth
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR
Bryan, Marian C.,Burdick, Daniel J.,Chan, Bryan K.,Chen, Yuan,Clausen, Saundra,Dotson, Jennafer,Eigenbrot, Charles,Elliott, Richard,Hanan, Emily J.,Heald, Robert,Jackson, Philip,La, Hank,Lainchbury, Michael,Malek, Shiva,Mann, Sam E.,Purkey, Hans E.,Schaefer, Gabriele,Schmidt, Stephen,Seward, Eileen,Sideris, Steve,Wang, Shumei,Yen, Ivana,Yu, Christine,Heffron, Timothy P.
supporting information, p. 100 - 104 (2016/02/03)
The rapid advancement of a series of noncovalent inhibitors of T790M mutants of EGFR is discussed. The optimization of pyridone 1, a nonselective high-throughput screening hit, to potent molecules with high levels of selectivity over wtEGFR and the broader kinome is described herein.
Purification and characterization of an NADH-dependent alcohol dehydrogenase from Candida maris for the synthesis of optically active 1-(pyridyl)ethanol derivatives
Kawano, Shigeru,Yano, Miho,Hasegawa, Junzo,Yasohara, Yoshihiko
experimental part, p. 1055 - 1060 (2012/02/03)
A novel (R)-specific alcohol dehydrogenase (AFPDH) produced by Candida maris IFO10003 was purified to homogeneity by ammonium sulfate fractionation, DEAE-Toyopearl, and Phenyl-Toyopearl, and characterized. The relative molecular mass of the native enzyme was found to be 59,900 by gel filtration, and that of the subunit was estimated to be 28,900 on SDS-polyacrylamide gel electrophoresis. These results suggest that the enzyme is a homodimer. It required NADH as a cofactor and reduced various kinds of carbonyl compounds, including ketones and aldehydes. AFPDH reduced acetylpyridine derivatives, β-keto esters, and some ketone compounds with high enantioselectivity. This is the first report of an NADH-dependent, highly enantioselective (R)-specific alcohol dehydrogenase isolated from a yeast. AFPDH is a very useful enzyme for the preparation of various kinds of chiral alcohols.