Results 21 to 30 of about 51,383 (265)

Lead identification and structure-activity relationships of heteroarylpyrazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists [PDF]

, 2014
A knowledge-based library of aryl 2,3-dichlorophenylsulfonamides was synthesised and screened as human CCR4 antagonists, in order to identify a suitable hit for the start of a lead-optimisation programme.
Copley, R.C.B., Miah, A.H., O'Flynn, D., Percy, J.M., Procopiou, P.A.   +4 more
core   +1 more source

Current status of pyrazole and its biological activities

Journal of Pharmacy and Bioallied Sciences, 2016
Pyrazole are potent medicinal scaffolds and exhibit a full spectrum of biological activities. This review throws light on the detailed synthetic approaches which have been applied for the synthesis of pyrazole.
Mohd Javed Naim, Ozair Alam, Farah Nawaz, Md. Jahangir Alam, Perwaiz Alam   +4 more
doaj   +1 more source

3-(3-Chloroanilino)-1-(3,5-dimethyl-1Hpyrazol-1-yl)propan-1-one [PDF]

, 2009
In the molecule of the title compound, C14H16ClN3O, the benzene and pyrazole rings are oriented at a dihedral angle of 3.50 (3)°. In the crystal structure, intermolecular N-H...O hydrogen bonds link the molecules into chains.
Aamer Saeed, Shahid Hussain, Michael Bolte, Akarca, Allen, Blessing, Elguero, Eriksson, Escolar, Mella, Penning, Saeed, Sheldrick, Spek   +13 more
core   +1 more source

Crystal structure of 6-amino-4-(3-bromo-4-methoxyphenyl)-3-methyl-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile dimethyl sulfoxide monosolvate

Acta Crystallographica Section E: Crystallographic Communications, 2015
In the pyrazole molecule of the title solvate, C15H13BrN4O2·C2H6OS, the dihedral angle between the benzene ring and the mean plane of the dihydropyrano[2,3-c]pyrazole ring system [r.m.s deviation = 0.031 (2) Å] is 86.71 (14)°.
Sammer Yousuf, Huma Bano, Munira Taj Muhammad, Khalid Mohammed Khan   +3 more
doaj   +1 more source

Rational Design, Synthesis and Biological Evaluation of Pyrimidine-4,6-diamine derivatives as Type-II inhibitors of FLT3 Selective Against c-KIT. [PDF]

, 2018
FMS-like Tyrosine Kinase 3 (FLT3) is a clinically validated target for acute myeloid leukemia (AML). Inhibitors targeting FLT3 have been evaluated in clinical studies and have exhibited potential to treat FLT3-driven AML.
Bharate, Jaideep B, Ding, Lucky, Frett, Brendan, Lakkaniga, Naga Rajiv, Li, Hong-Yu, McConnell, Nicholas, Naresh, Gunaganti, Shah, Neil P, Zhang, Lingtian   +8 more
core   +2 more sources

Trispyrazolylborate Ligands Supported on Vinyl Addition Polynorbornenes and Their Copper Derivatives as Recyclable Catalysts [PDF]

, 2019
Polynorbornenes prepared by vinyl addition poly- merization and bearing pendant alkenyl groups serve as skeletons to support trispyrazolylborate ligands (Tpx) built at those alkenyl sites.
Albéniz Jiménez, Ana Carmen, Beltrán de Heredia Rentería, Juan, Díaz Requejo, María del Mar, Molina de la Torre, Jesús Ángel, Pérez Ortega, Ignacio, Pérez, Pedro J., Rodríguez, Manuel R.   +6 more
core   +2 more sources

Machine Learning Accelerates Crystallization for Structure Determination

Angewandte Chemie, EarlyView.
Single‐crystal x‐ray diffraction (SCXRD) is often constrained by the difficulty of obtaining suitable crystals. Here, a machine learning‐accelerated co‐crystal discovery workflow is established for a crystalline mate strategy that achieves over 95% prediction accuracy and experimentally delivers 114 co‐crystals from 120 candidates.
Cui‐Zhou Luan, Xue‐Zhi Wang, Jian‐Guo Song, Yu Gu, Jing Wu, Ye‐Ting Wang, Jin‐Feng Liang, Jia‐Le Rao, Mo Xie, Jonathan R. Nitschke, Dan Li   +10 more
wiley   +2 more sources

{2,6-Bis[(2,6-diisopropylphosphanyl)oxy]-4-fluorophenyl-κ3P,C1,P′}(1H-pyrazole-κN2)nickel(II) hexafluorophosphate

Acta Crystallographica Section E, 2012
The title compound, [Ni(C18H30FO2P2)(C3H4N2)]PF6, was prepared by halide abstraction with TlPF6 in the presence of CH3CN in CDCl3 from the respective neutral pincer chlorido analogue followed by addition of pyrazole.
Man-Lung Kwan, Sara J. Conry, Charles S. Carfagna, Loren P. Press, Oleg V. Ozerov, Norris W. Hoffman, Richard E. Sykora   +6 more
doaj   +1 more source

Synthesis, biological evaluation, and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis: Part 2. Synthesis of rigid pyrazolones [PDF]

, 2009
Two series of novel rigid pyrazolone derivatives were synthesized and evaluated as inhibitors of Mycobacterium tuberculosis (MTB), the causative agent of tuberculosis. Two of these compounds showed a high activity against MTB (MIC = 4 μg/mL).
Alessandro De Logu, Beatrice Bechi, Biava, Biava, Biava, Brock, Castagnolo, Daniele Castagnolo, De Logu, Deidda, Fabrizio Manetti, Gutierrez-Lugo, Holzer, Janin, Mafalda Pagano, Manetti, Manuela Saddi, Marco Radi, Maurizio Botta, Rita Meleddu   +19 more
core   +1 more source

Deprotonative C(sp3)/C(sp2)–H (Multi)Silylation of (Hetero)Arenes Mediated by NaTMP

Angewandte Chemie, EarlyView.
An operationally simple protocol using a strongly basic sodium amide in combination with sterically emcumbered silicon electrophiles enables the deprotonative C–H (multi)silylation of a myriad of (hetero)arenes. Mechanistic investigations highlight the pivotal role of steric and coordination effects in controlling the regioselectivity and efficiency of
David Sánchez‐Roa, Sophia Belrhomari, Ana McGinley, Clevin Anto Liju, Manting Mu, Max García‐Melchor, Eva Hevia   +6 more
wiley   +2 more sources