Results 51 to 60 of about 12,908,442 (282)

1‐Azabicyclo[1.1.0]butanes (ABBs) on the Map: Mechanistic Pathways for Catalytic Ring Opening and Functionalizations

Angewandte Chemie, EarlyView.
Catalytic strain‐release ring opening and functionalizations of 1‐azabicyclo[1.1.0]butanes (ABBs) represent a promising strategy for accessing diverse azetidine products. These transformations proceed via polar pathways, radical pathways, and hybrid mechanisms that combine both.
James Shao‐Jiun Yang, Hsuan‐Hung Liao   +1 more
wiley   +2 more sources

A New Recruitable E3 Ligase UHRF1 Supporting Targeted Protein Degradation: A Minimal Azide as a Recruitment Ligand

Advanced Science, EarlyView.
Targeted protein degradation is often limited by the scarcity of usable E3 ligases. Herein, we report the first small‐molecule GPX4 degraders that incorporate either electrophilic warheads or a minimal azide group as an E3 recruitment ligand. The azide‐based degrader DK‐5070 effectively drives potent GPX4 degradation; mechanistic studies reveal that ...
Zehong Lin, Kang Duan, Rui Wan, Tao Jiang, Jinzhe Wei, Miao Sun, Mariia A. Skryl'nikova, Maxim A. Gureev, Zhi‐Min Zhang, Zhang Zhang, Ke Ding, Nan Ma, Tongzheng Liu, Yi Tan, Zhengqiu Li   +14 more
wiley   +1 more source

Unveiling the Complete Biosynthetic Pathway of Azacitidine: A Rare 1,3,5‐Triazine Nucleoside Derived From GTP

Angewandte Chemie, EarlyView.
The azacitidine biosynthetic gene cluster (aza BGC) was identified by the resistance‐gene‐guided comparative genomics method in Streptomyces mobaraensis IPIO2. The complete biosynthetic pathway of azacitidine, which follows a “base‐first‐then‐glycosylation” logic, was elucidated through in vivo and in vitro experiments.
Dan Wang, Qingxu Meng, Lingqi Hua, Mengjun Sun, Qianjin Kang, Min‐Juan Xu, Linquan Bai   +6 more
wiley   +2 more sources

1-(4-Nitrophenyl)-1H-1,2,3-Triazole-4-carbaldehyde: Scalable Synthesis and Its Use in the Preparation of 1-Alkyl-4-Formyl-1,2,3-triazoles

Organics, 2021
1,2,3-Triazole-4-carbaldehydes are useful synthetic intermediates which may play an important role in the discovery of novel applications of the 1,2,3-triazole moiety.
Tomas Opsomer, Kaat Valkeneers, Ana Ratković, Wim Dehaen   +3 more
doaj   +1 more source

AS‐TLC‐Based High‐Throughput Screening Integrated with CuAAC Optimization Strategy Facilitates the Rapid Discovery of YTHDC1 Inhibitor

Advanced Science, EarlyView.
We developed Affinity Selection Thin‐Layer Chromatography (AS‐TLC) as a method for high‐throughput screening (HTS) of compound mixtures. Furthermore, we integrated activity assays with AS‐TLC and identified a YTH domain‐containing protein 1 (YTHDC1) inhibitor. Building on this hit, we applied copper(I)‐catalyzed azide–alkyne cycloaddition (CuAAC) click
Mingchen Wang, Shuiping Fu, Ye Xu, Jia Gao, Jiwei Ren, Xu Yang, Hesong Xu, Ge Sun, Yanjie Li, Yanlin Wang, Lu Jin, Peijuan Chen, Ying Xu, Jianhao Li, Hua Lin, Chujiao Hu, Kaixian Chen, Huan Xiong, Cheng Luo, Shijie Chen   +19 more
wiley   +1 more source

Site‐Specific Protein Bioconjugation Through Cellular Incorporation of Noncanonical Amino Acids

Angewandte Chemie, EarlyView.
Genetic code expansion (GCE) enables site‐specific installation of noncanonical amino acids containing bioorthogonal conjugation handles, allowing precise, homogeneous protein modification. This review examines the principles of orthogonal translation, surveys the chemistries available for chemoselective labeling, and highlights emerging multi‐site ...
Rahul Sarkar, Manas Joshi, Abhishek Chatterjee   +2 more
wiley   +2 more sources

Regioselective formation of new 3-S-alkylated-1,2,4-triazole-quinolones

, 2021
Regioselective synthesis of quinolone-1,2,4-triazoles was established starting from 4-hydroxyquinol-2-ones. The strategy started by the reaction of ethyl bromoacetate with 4-hydroxyquinoline to give the corresponding ethyl oxoquinolinyl acetates, which ...
Alan B. Brown (11775964), Yaseen A.M.M. Elshaier (11775961), Martin Nieger (1628914), Mohamed Ramadan (3633547), Hazem M. Fathy (11775967), Ashraf A. Aly (3184356), Stefan Bräse (2454700), Mohamed Abd El-Aziz (11775958)   +7 more
core   +1 more source

Sequential Patterning of Photoresponsive Hydrogels Directs Crypt Fission and Reveals the Role of Epithelial Curvature on Fission Symmetry

Advanced Science, EarlyView.
Deterministic crypt fission is achieved in intestinal organoids using photopatternable hydrogels with spatiotemporal control. Daughter‐crypt symmetry is shown to depend on parent‐crypt geometry and epithelial curvature, while myosin‐dependent mechanosensing links tissue shape to regenerative outcomes.
Delaney L. McNally, Kaustav Bera, Nolan R. Petrich, Alex Khang, Marilyne Coulombe, David Castillo‐Azofeifa, Ophir D. Klein, Peter J. Dempsey, Kristi S. Anseth   +8 more
wiley   +1 more source

SOLiD‐MaP: A Photoproximity Labeling Platform for Small Molecule Binding Site Mapping on RNA

Angewandte Chemie, EarlyView.
SOLiD‐MaP is a ligand‐directed photoproximity labeling strategy developed for RNA binding‐site analysis. Singlet oxygen‐mediated labeling creates a proximity‐dependent chemical footprint of bound small molecules on RNA. Coupling this chemistry with mutational profiling enables identification of the ligand‐binding region at nucleotide resolution ...
Lin L. Rietveld, Wei Wu, Filip M. Zawisza, Danny Incarnato, Zeshi Li   +4 more
wiley   +2 more sources

Synthesis, physical-chemical properties of 2-((4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-yl)thio)acetohydrazides

Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki, 2017
Aim. Analysis of the scientific literature over the past decade has shown that large synthetic possibilities towards creating new and effective drug substances have heterocyclic compounds, in particular the derivatives of 1,2,4-triazole.
O. A. Suhak, O. I. Panasenko, Ye. G. Knysh   +2 more
doaj   +1 more source