Results 51 to 60 of about 15,176 (256)

Diastereoselective Synthesis of 2‑Phenyl-3-(trifluoromethyl)piperazines as Building Blocks for Drug Discovery

, 2016
The synthesis of enantiomerically pure cis- and trans-2-phenyl-3-(trifluoromethyl)­piperazines is described. It involved, as the key step, a diastereoselective nucleophilic addition of the Ruppert–Prakash reagent (TMSCF3) to α-amino sulfinylimines ...
Santos Fustero (1330944), Andrés A. Trabanco (1463707), Michiel Van Gool (1367739), Oscar Delgado (1367715), Natalia Mateu (1789096), María Sánchez-Roselló (1490935)   +5 more
core   +1 more source

SPHINX31 acts as a SRPK1 inhibitor targeting the ATR/DNA‐PKcs/CHK1 replicative checkpoint to inhibit cell growth in non‐small cell lung cancer

Molecular Oncology, EarlyView.
The kinase SRPK1 directly interacts with the protein TOPBP1 and regulates the pre‐mRNA splicing of WIZ thereby contributing to the activation of the ATR/CHK1 replicative checkpoint in response to replicative stress. This allows cancer cells' genomic stability and survival.
Amani Shreim, Aurelie Genoux, Nadiia Zubchuk, Haoyang Zheng, Perla Salameh, Theo Ziegelmeyer, Fabien Dalonneau, Margot Rouchette, Christiane Oddou, Simona Miron, Helene Polveche, Adiilah Mamode Cassim, Carmen Garrido, Eleni Nikolakaki, Didier Auboeuf, Tao Jia, Sophie Zinn‐Justin, Beatrice Eymin   +17 more
wiley   +1 more source

Iridium catalysed synthesis of piperazines from diols

, 2007
A green and atom-economical method has been developed for the synthesis of piperazines by cyclocondensation of diols and amines in aqueous media in the presence of a catalytic amount of [Cp*IrCl2 ...
Madsen, Robert, Nordstrøm, Lars Ulrik Rubæk   +1 more
core   +1 more source

A Holistic Platform Approach for Developing Robust Pulmonary mRNA Delivery: Integrating Novel Phenolic Acid‐Derived Ionizable Lipids and Device Engineering

Advanced Functional Materials, EarlyView.
An integrated pulmonary mRNA delivery platform combining novel biodegradable syringic acid‐derived ionizable lipids, design‐of‐experiments formulation optimization, and vibrating‐mesh nebulizer engineering enabled stable aerosolization and efficient lung delivery.
Neha Kaushal, Younan Ma, Asad Khanmohammed, Dipen Parande, Hanming Zhang, Saket Dolare, Juliet Chen, Apiwat Wangweerawong, Saswata Karmakar, Hongfeng Deng, Frank Koppenhagen, Shraddha Sharma, Eric Reyes, Sherry He, Lianne Boeglin, Caroline Woo, Azadeh Paksa, Ayed Allawzi, Anusha Dias, Gregory Troiano, Shrirang Karve, Frank DeRosa   +21 more
wiley   +1 more source

Proximity‐Induced Protein Deglycosylation by Endogenous O‐GlcNAcase

Angewandte Chemie, EarlyView.
Bifunctional molecules recruit endogenous O‑GlcNAcase to target proteins, enabling selective de‑O‑GlcNAcylation in living cells without perturbing global O‑GlcNAc homeostasis. This work developed a programmable chemical strategy for targeted O‑GlcNAc editing and framework for functional enzymatic recruitment via optimization of competitive enzyme ...
Haixing Xu, Bowen Ma, Yunpeng Huang, Jialin Liu, Billy Wai‐Lung Ng   +4 more
wiley   +2 more sources

Synthesis of 2,6-Disubstituted Piperazines by a Diastereoselective Palladium-Catalyzed Hydroamination Reaction

, 2016
A highly diastereoselective intramolecular hydroamination is the key step in a modular synthesis of 2,6-disubstituted piperazines. The requisite hydroamination substrates were prepared in excellent yields by nucleophilic displacement of cyclic ...
Forrest E. Michael (1872319), Brian M. Cochran (2411149)   +1 more
core   +2 more sources

Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion

, 2021
Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic ...
Tania De Koning-Ward (13096974), HJ Sabroux (14461746), PR Gilson (9074540), W Nguyen (13462635), MG Dans (14461737), KN Lowes (14461743), BE Sleebs (14461755), VM Avery (14461749), S Duffy (7707776), DW Wilson (14461752), A Ngo (9854420), O Romeo (13410972), MR Gancheva (14461740)   +12 more
core  

Nickel‐Catalyzed Three‐Component Difluoroalkylation‐Amination for the Direct Access to Anti‐Inflammatory β‐Difluoroalkyl Amines

Advanced Science, EarlyView.
A nickel‐catalyzed three‐component reductive fluoroalkylation‐amination strategy of N‐vinylamides for the direct access to the α‐amidyl‐β‐difluoroalkyl amines was reported here. The synthetic method features with broad substrate scope, mild conditions, high functional group tolerance, and convenience to handle.
Chang Xu, Fangting Ma, Fan Ding, Luyan Wang, Yunxi Li, Yunzhi He, Xingang Zhang, Siyu He, Dandan Liu   +8 more
wiley   +1 more source

Hydrogen‐Bonding Order Associated With Radical Delocalization in Layered Organic Cathode Materials

Angewandte Chemie, EarlyView.
“TAQ” and TAPT share the same pyrazine‐based molecular structure but differ in degree of crystallinity. Combined x‐ray scattering, solid‐state NMR, MicroED, and EPR reveal that “TAQ”'s higher crystallinity and ordered hydrogen‐bonding network are associated with enhanced radical delocalization and conductivity, highlighting structural order as a design
Alae Eddine Lakraychi, Zeqian Zhang, Oliver Lin, Eric D Walter, Jiaqi Wang, Harshan Reddy Gopidi, Eliot F. Woods, Ruozhu Feng, Wei Wang, Pieremanuele Canepa, Brett A. Helms, Kamila M. Wiaderek, Qian Chen, Yan Yao, Ying Chen   +14 more
wiley   +2 more sources

A Small‐Molecule DEPTAC Rescues Cognitive Deficits by Targeted Dephosphorylation of Pathological Tau

Advanced Science, EarlyView.
TP2 is a fully synthetic small‐molecule dephosphorylation‐targeting chimera that recruits endogenous PP2A‐Bα to Tau, enabling targeted removal of pathological phosphate modifications. In two tauopathy mouse models, systemic TP2 reduces Tau pathology, preserves neuronal and synaptic integrity, improves neuroimmune homeostasis, and rescues cognition ...
Fei Sun, Yang Liu, Qiuzhi Zhou, Qingyuan Hu, Weixia Wang, Yue Xiao, Jingfen Su, Guanting Liu, Miaomiao Sun, Lixia Chen, Hua Li, Ying Yang, Jian‐Zhi Wang   +12 more
wiley   +1 more source