نتایج جستجو برای: pyridinyl

تعداد نتایج: 490  

Journal: :ACS medicinal chemistry letters 2010
Steven D Knight Nicholas D Adams Joelle L Burgess Amita M Chaudhari Michael G Darcy Carla A Donatelli Juan I Luengo Ken A Newlander Cynthia A Parrish Lance H Ridgers Martha A Sarpong Stanley J Schmidt Glenn S Van Aller Jeffrey D Carson Melody A Diamond Patricia A Elkins Christine M Gardiner Eric Garver Seth A Gilbert Richard R Gontarek Jeffrey R Jackson Kevin L Kershner Lusong Luo Kaushik Raha Christian S Sherk Chiu-Mei Sung David Sutton Peter J Tummino Ronald J Wegrzyn Kurt R Auger Dashyant Dhanak

Phosphoinositide 3-kinase α (PI3Kα) is a critical regulator of cell growth and transformation, and its signaling pathway is the most commonly mutated pathway in human cancers. The mammalian target of rapamycin (mTOR), a class IV PI3K protein kinase, is also a central regulator of cell growth, and mTOR inhibitors are believed to augment the antiproliferative efficacy of PI3K/AKT pathway inhibiti...

Journal: :Chemical & pharmaceutical bulletin 2002
Hidemitsu Nishida Yutaka Miyazaki Takafumi Mukaihira Fumihiko Saitoh Miyuki Fukui Kousuke Harada Manabu Itoh Aki Muraoka Tomokazu Matsusue Atsushi Okamoto Yoshitaka Hosaka Miwa Matsumoto Shuhei Ohnishi Hidenori Mochizuki

Intravascular clot formation is an important event in a number of cardiovascular diseases. The prevention of blood coagulation has become a major target for new therapeutic agents. Factor Xa (FXa) is a trypsin-like serine protease that plays a key role in the blood coagulation cascade and represents an attractive target for anticoagulant drug development. We have investigated substituents in th...

Journal: :Dalton transactions 2013
Jacky Pouessel Sabah Abada Nathalie Le Bris Mourad Elhabiri Loïc J Charbonnière Raphaël Tripier

The synthesis of a new linear bis-tetraamine ligand L1, based on two 1,4,8,11-tetraazaundecane units grafted at the 2 and 6 positions of a pyridinyl linker substituted by an anthracenyl fluorophore in the para position, is described and anion complexation studies of L1 with anionic substrates are reported. The protonation pattern and the study of the binding properties of L1 in an aqueous mediu...

2008
Pierre Koch Christiane Bäuerlein Dieter Schollmeyer Stefan Laufer

The title compound, C(19)H(18)FN(3)O(2)S, was synthesized in the course of studies on 2-alkyl-sufanylimidazoles as p38 mitogen-activated protein kinase inhibitors. The synthesis was achieved by nucleophilic substitution of 4-(4-fluoro-phen-yl)-5-(pyridin-4-yl)-1,3-dihydro-imidazole-2-thione with methyl 4-bromo-butanoate. The five-membered heterocycle makes dihedral angles of 32.4 (2) and 18.3 (...

Journal: :Molecules 2014
Jean I du Toit Margaritha Jordaan Carlijn A A Huijsmans Johannes H L Jordaan Cornelia G C E van Sittert Hermanus C M Vosloo

Hemilabile ligands can release a free coordination site "on demand" of an incoming nucleophilic substrate while occupying it otherwise. This is believed to increase the thermal stability and activity of catalytic systems and therefore prevent decomposition via free coordination sites. In this investigation chelating pyridinyl-alcoholato ligands were identified as possible hemilabile ligands for...

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