Results 31 to 40 of about 47,847 (251)

Carbohydrate‐Directed Labeling Probes for UV‐Independent Chemoproteomic Profiling of Carbohydrate–Protein Interactions

Angewandte Chemie, EarlyView.
Modular carbohydrate‐directed labeling probes (CDLPs) convert weak carbohydrate–protein interactions into durable covalent tags in live cells without the need for multivalency or UV irradiation. Ligand binding triggers proximity‐enabled, glycan‐releasing acyl transfer to install a click handle for protein tagging and chemoproteomic profiling.
Matthew C. Russolillo, Wariya Nirachonkul, Nora Ross, Rahul M. Hedau, Zachary Clark, Michaella J. Rekowski, Michael P. Washburn, Mark P. Farrell   +7 more
wiley   +2 more sources

Anticonvulsant activity 2-((5-(3-(4-fluorophenyl)-4-R2-1,2,4-triazole-3-yl)-thio)-1-arylethanone

Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki, 2019
The aim of work is to study of the anticonvulsant activity of 2-((5-(3-,4-fluorophenyl)-4-R2-1,2,4-triazole-3-yl)thio)-1-aryletanones, the establishment of some laws between the structure of compounds and their activity. Materials and methods.
O. A. Bihdan
doaj   +1 more source

Synthesis and alkylation of 5-aryl-1,2-dihydro-3H-1,2,4-triazole-3-thiones

Журнал органічної та фармацевтичної хімії, 2021
5-R-1,2,4-triazole-3-thiones and their derivatives are easy to obtain; they have low toxicity and a broad spectrum of the biological activity. It makes this class of heterocyclic compounds promising for creating potential drugs. Aim.
Dmytro V. Dovbnya, Andrii G. Kaplaushenko, Alla S. Korzhova   +2 more
doaj   +1 more source

Functional Sex Reversal in Adult Gonochoristic Teleosts is Mediated by Ovarian Germline Stem Cell Plasticity and Somatic Cell Transdifferentiation

Advanced Science, EarlyView.
Oocytes play crucial roles in maintaining ovarian fate in adult gonochoristic fish. Targeted oocyte ablation with aromatase inhibition triggers the activation of surviving germline stem cells and the transdifferentiation of somatic cells from granoulosa/theca to Sertoli/Leydig lineages, inducing a complete and functional female‐to‐male sex reversal ...
Yang Yang, Liechao Yu, Wanchang Zhang, Gary Wessel, Ruiyi Chen, Weihua Hu, Dongdong Xu   +6 more
wiley   +1 more source

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

Acute toxicity of 5-(furan-2-yl, 2-metylfuran-3-yl)-4-amino-1,2,4-triazole-3-thiol alkyl derivatives

Zaporožskij Medicinskij Žurnal, 2017
The purpose of our work was the further exploration of the new 5-(furan-2-yl, 2-metylfuran-3-yl)-4-amino-1,2,4-triazole-3-thiol alkyl derivatives’ acute toxicity, setting some patterns of alkyl substituents influence by the Sulfur atom on the acute ...
D. M. Danilchenko, V. V. Parchenko
doaj   +1 more source

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

Design, Molecular Docking Studies and Toxicity Prediction of Some Novel 1, 2, 3-Triazole Derivatives Containing Piperazine Moiety as Antifungal Agents and CYP-51 Inhibitors [PDF]

Journal of Advanced Biomedical Sciences, 2018
Background & Objective: In this study, a number of new triazole derivatives, containing a 1, 2, 3-triazole ring attached to the piperazine moiety as antifungal agents and lanosterol 14 alpha-demethylase, (CYP51) inhibitors were docking studies conducted.
abozar roeintan, Fatemeh Fadaei Nobandegani   +1 more
doaj  

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