Results 71 to 80 of about 53,373 (308)

The pyrazolo[4,3-c]pyrazole core as a novel and versatile scaffold for developing dual DYRK1A-CLK1 inhibitors targeting key processes of Alzheimer's disease pathology

European Journal of Medicinal Chemistry Reports
In the current study, we designed, synthesized, and characterized a series of substituted pyrazolo[4,3-c]pyrazoles. These novel compounds were evaluated in vitro for their inhibitory activity over a panel of protein kinases to determine their potential ...
Vaia-Argyro Bakalakou, Barbara Mavroidi, Amalia D. Kalampaliki, Béatrice Josselin, Stéphane Bach, Alexios-Leandros Skaltsounis, Panagiotis Marakos, Nicole Pouli, Maria Pelecanou, Vassilios Myrianthopoulos, Sandrine Ruchaud, Ioannis K. Kostakis   +11 more
doaj   +1 more source

An Example of Polynomial Expansion: The Reaction of 3(5)-Methyl-1H-Pyrazole with Chloroform and Characterization of the Four Isomers

Molecules, 2019
The reaction in phase-transfer catalyzed conditions of 3(5)-methyl-1H-pyrazole with chloroform affords four isomers 333, 335, 355 and 555 in proportions corresponding to the polynomial expansion (a + b)3, with a = 0.6 and b = 0.4, a and b being 3-methyl ...
Vera L. M. Silva, Artur M. S. Silva, Rosa M. Claramunt, Dionisia Sanz, Lourdes Infantes, Ángela Martínez-López, Felipe Reviriego, Ibon Alkorta, José Elguero   +8 more
doaj   +1 more source

Thinking Outside the Binding Site: A Self‐Encapsulating Kinase Inhibitor Remodels Its Pocket to Achieve Selectivity

Angewandte Chemie International Edition, EarlyView.
To make exceptionally effective drugs, thinking “outside the binding site” is required. This work reveals that counterintuitive targeting of a kinase‐conserved region can lead to highly selective binding. Inhibitor discovery coupled to x‐ray crystallography shows that a network of noncanonical interactions and long‐range effects of distant unique amino
Nico J. Seidler, Monica R. MacDonald, Athina A. Moschopoulou, Sahba Cunningham, Tess M. Weber, Nader N. Nasief, Lorenz Mayer, Frederik W. Hacker, Ekaterina Hermann, Mareike B. Möllers, Yuliia Skliarenko, Tahereh Damghani, Abid N. Manzar, Kaly S. Lin, Ramona Rudalska, Marcia I. Goettert, Lars Zender, Daniel Dauch, Michael Forster, Stefan A. Laufer, David E. Heppner   +20 more
wiley   +1 more source

Temperature-Controlled Divergent Synthesis of Pyrazoles and 1-Tosyl-1H-pyrazoles under Transition-Metal-Catalyst- and Oxidant-Free Conditions

Molecules
Herein, a general and practical temperature-controlled approach for the divergent synthesis of pyrazoles and 1-tosyl-1H-pyrazoles via electrophilic cyclization in the absence of transition-metal catalysts and oxidants was developed.
Kai Wang, Wenjing Xu, Chengcai Xia, Xianting Cao   +3 more
doaj   +1 more source

Drug-Clinical Agent Molecular Hybrid: Synthesis of Diaryl(trifluoromethyl)pyrazoles as Tubulin Targeting Anticancer Agents

ACS Omega, 2018
Twenty-three combretastatin A-4 (CA-4) analogues were synthesized by judiciously incorporating a functional N-heterocyclic motif present in Celecoxib (a marketed drug) while retaining essential pharmacophoric features of CA-4.
Neha Hura, Afsana Naaz, S. Prassanawar, S. Guchhait, D. Panda   +4 more
semanticscholar   +1 more source

A new route to the synthesis of imidazo [4,5-c]pyrazoles

, 1988
A new synthesis of imidazo [4,5-c] pyrazoles, obtained through cyclisation of 4-nitroso-5-alkylamino-pyrazoles, is described ...
GIORI, Paolo, VERONESE, Augusto, Augusto Cesare Veronese, VICENTINI, Chiara Beatrice, Chiara Beatrice Vicentini, Paolo Giori, GUARNERI, Mario, Mario Guarneri   +7 more
core   +1 more source

Extending Peptide Ligation to Acidic pH and Junctions Comprising Glycosylated and Phosphorylated Amino Acids

Angewandte Chemie International Edition, EarlyView.
A pyridine‐containing ligation auxiliary eliminates a major bottleneck of peptide ligation chemistry. The extended range of applicable pH values (2.0–7.5) in the ligation reaction helps to avoid epimerization. Native chemical ligation (NCL) proceeds at virtually any junction, including reactions at β‐branched amino acids, as well as O‐glycosylated or O‐
Sebastian Trunschke, Antonia Feida, Hendrik Hanebrink, Arseniy Galashov, Alina Herfort, Oliver Seitz   +5 more
wiley   +1 more source

Synthesis of 4-functionalized pyrazoles via oxidative thio- or selenocyanation mediated by PhICl2 and NH4SCN/KSeCN

Beilstein Journal of Organic Chemistry
A series of 4-thio/seleno-cyanated pyrazoles was conveniently synthesized from 4-unsubstituted pyrazoles using NH4SCN/KSeCN as thio/selenocyanogen sources and PhICl2 as the hypervalent iodine oxidant.
Jialiang Wu, Haofeng Shi, Xuemin Li, Jiaxin He, Chen Zhang, Fengxia Sun, Yunfei Du   +6 more
doaj   +1 more source

Synthesis of Novel Pyrazole Derivatives and Their Tumor Cell Growth Inhibitory Activity

Molecules, 2019
To find novel antitumor agents, a series of 1H-benzofuro[3,2-c]pyrazole derivatives 4a-e were designed and synthesized. The treatment of 6-methoxybenzofuran-3(2H)-one 3 with LiHMDS in anhydrous tetrahydrofuran (THF) followed by reaction with 3-substitued
Ying-Jie Cui, Long-Qian Tang, Cheng-Mei Zhang, Zhao-Peng Liu   +3 more
doaj   +1 more source

Pyrazoles as Key Scaffolds for the Development of Fluorine-18-Labeled Radiotracers for Positron Emission Tomography (PET)

Molecules, 2020
The need for increasingly personalized medicine solutions (precision medicine) and quality medical treatments, has led to a growing demand and research for image-guided therapeutic solutions.
Pedro M. O. Gomes, Artur M. S. Silva, Vera L. M. Silva   +2 more
doaj   +1 more source