نتایج جستجو برای: 2 aminothiazole

تعداد نتایج: 2525278  

Journal: :Molecular cancer therapeutics 2014
Christine Fritsch Alan Huang Christian Chatenay-Rivauday Christian Schnell Anupama Reddy Manway Liu Audrey Kauffmann Daniel Guthy Dirk Erdmann Alain De Pover Pascal Furet Hui Gao Stephane Ferretti Youzhen Wang Joerg Trappe Saskia M Brachmann Sauveur-Michel Maira Christopher Wilson Markus Boehm Carlos Garcia-Echeverria Patrick Chene Marion Wiesmann Robert Cozens Joseph Lehar Robert Schlegel Giorgio Caravatti Francesco Hofmann William R Sellers

Somatic PIK3CA mutations are frequently found in solid tumors, raising the hypothesis that selective inhibition of PI3Kα may have robust efficacy in PIK3CA-mutant cancers while sparing patients the side-effects associated with broader inhibition of the class I phosphoinositide 3-kinase (PI3K) family. Here, we report the biologic properties of the 2-aminothiazole derivative NVP-BYL719, a selecti...

Journal: :The Journal of pharmacology and experimental therapeutics 2002
Danielle Gully Michel Geslin Laurence Serva Evelyne Fontaine Pierre Roger Christine Lair Valerie Darre Claudine Marcy Pierre-Eric Rouby Jacques Simiand Josette Guitard Georgette Gout Regis Steinberg Daniel Rodier Guy Griebel Philippe Soubrie Marc Pascal Rebecca Pruss Bernard Scatton Jean-Pierre Maffrand Gerard Le Fur

4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1- (3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A), a new 2-aminothiazole derivative, shows nanomolar affinity for human cloned or native corticotrophin-releasing factor (CRF)(1) receptors (pK(i) values of 8.73 and 9.08, respectively), and a 1000-fold selectivity for CRF(1) versus C...

Journal: :Analytical sciences : the international journal of the Japan Society for Analytical Chemistry 2004
Ilton L Alcântara Paulo S Roldan Gustavo R Castro Fabrício V Moraes Fábio A Silva Cilene C F Padilha Jorge D Oliveira Pedro M Padilha

A rapid and sensitive method was developed to determine trace levels of Cd2+ ions in an aqueous medium by flame atomic absorption spectrometry, using on-line preconcentration in a mini-column packed with 100 mg of 2-aminothiazol modified silica gel (SiAT). The Cd2+ ions were sorbed at pH 5.0. The preconcentrated Cd2+ ions were directly eluted from the column to the spectrometer's nebulizer-burn...

Journal: :Acta Crystallographica Section D: Biological Crystallography 2007
Günter Pappenberger Tanja Schulz-Gasch Eric Kusznir Francis Müller Michael Hennig

Fatty-acid synthesis in bacteria is of great interest as a target for the discovery of antibacterial compounds. The addition of a new acetyl moiety to the growing fatty-acid chain, an essential step in this process, is catalyzed by beta-ketoacyl-ACP synthase (KAS). It is inhibited by natural antibiotics such as cerulenin and thiolactomycin; however, these lack the requirements for optimal drug ...

Journal: :The Journal of antibiotics 1984
E Perrone M Alpegiani F Giudici F Buzzetti G Nannini G Meinardi S Grasso A Bianchi I de Carneri

Introduction of a hydroxyl group into the thiazole ring nitrogen of cephalosporins belonging to the cefotiam and cefotaxime families gave rise to products, better described by the tautomeric N-oxide form, which proved particularly active against Gram-negative bacteria. Cephems bearing a (Z)-alkoxyimino functionality are of special interest for broadness of spectrum; among them, 7 beta-[(Z)-2-(2...

Journal: :Chemical Engineering Journal 2022

• Functionalization of magnetic-chitosan microparticles for chromate removal. High efficiency and selectivity imidazole carboxamide derivative. Sorption capacities as high 6 mmol Cr g −1 , at pH 2 (including Cr(VI) reduction). Sips pseudo-first order rate equations isotherm kinetic fitting, resp. Highly efficient desorption with 0.5 M HCl sorbent recycling (5 cycles). Textile tannery industries...

2014
Christine Fritsch Alan Huang Christian Chatenay-Rivauday Christian Schnell Anupama Reddy Manway Liu Audrey Kauffmann Daniel Guthy Dirk Erdmann Alain De Pover Pascal Furet Hui Gao Stephane Ferretti Youzhen Wang Joerg Trappe Saskia M. Brachmann Sauveur-Michel Maira Christopher Wilson Markus Boehm Carlos Garcia-Echeverria Patrick Chene Marion Wiesmann Robert Cozens Joseph Lehar Robert Schlegel Giorgio Caravatti Francesco Hofmann William R. Sellers

Somatic PIK3CA mutations are frequently found in solid tumors, raising the hypothesis that selective inhibition of PI3Kamay have robust efficacy in PIK3CA-mutant cancers while sparing patients the side-effects associated with broader inhibition of the class I phosphoinositide 3-kinase (PI3K) family. Here, we report the biologic properties of the 2-aminothiazole derivative NVP-BYL719, a selectiv...

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