Results 41 to 50 of about 11,349 (193)

Strategic application of CuAAC click chemistry in the modification of natural products for anticancer activity

European Journal of Medicinal Chemistry Reports, 2023
Natural products play a key role in the history of human drug discovery, and especially for the anticancer agents. Copper(I)-catalyzed alkyne-azide [3+2] cycloaddition (CuAAC) reaction is perhaps the most powerful method for the efficient modification of
Zaozao Xiao, Yuang Gu, Hewei Dong, Bo Liu, Weiwei Jin, Jie Li, Peixiang Ma, Hongtao Xu, Wei Hou   +8 more
doaj   +1 more source

Synthesis and CuAAC Reactions of Azidoalkylethoxysilanes: Grafting CuAAC Products onto Silica Surface

, 2014
One-pot synthetic protocols of novel azido functionalized silane coupling agents from corresponding terminal mesylated or tosylated 1-olefins were developed.
Roman G. Kultyshev (526315), Akira Miyazawa (526318), Yuji Kawanishi (526316), Masateru Nishioka (526317)   +3 more
core   +1 more source

Multiplexed CuAAC Suzuki–Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling

, 2021
Mass-spectrometry-based chemoproteomics has enabled the rapid and proteome-wide discovery of functional and potentially 'druggable' hotspots in proteins.
Castellón, José O, Chan, Neil J, Boatner, Lisa M, Desai, Heta S, Cao, Jian, Burton, Nikolas R, Armenta, Ernest, Backus, Keriann M, Neil J. Chan, Lisa M. Boatner, Heta S. Desai, Nikolas R. Burton, Jian Cao, Ernest Armenta, Keriann M. Backus, José O. Castellón   +15 more
core   +1 more source

IMPDH inhibition enhances cytarabine efficacy in SAMHD1‐expressing leukaemia cells via guanine nucleotide depletion

Molecular Oncology, EarlyView.
Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla, Christopher Dirks, Caroline Eiden, Sonja K. Fesenmayer, Femke M. Hormann, Yolande Klootsema, Ingrid Lilienthal, Si Min Zhang, Nikolas Herold, Sean G. Rudd   +9 more
wiley   +1 more source

Molecular Glue Degraders of TEM β‐Lactamases by Periplasmic Protease DegP

Angewandte Chemie, EarlyView.
Molecular glues are developed that target TEM‐family β‐lactamases to the bacterial protease DegP for degradation. β‐Lactamase inhibitor tazobactam is identified as accelerating TEM β‐lactamase degradation by DegP, which is further enhanced by linkerless incorporation of dipeptides enriched among DegP substrates.
Emilia K. Taylor, Patricia Santos Barbosa, Tarini Kadambi, Frederik Eisele, Yiqiao Wang, Elisabete C. C. M. Moura, Timothy R. Walsh, Georgia L. Isom, Thomas Lanyon‐Hogg   +8 more
wiley   +2 more sources

Poly(Alkoxythiophene) Rod‐Coil Block Copolymers for Organic Electrochemical Transistors

Advanced Materials, EarlyView.
We present the first synthesis of poly(3‐alkoxythiophene) rod‐coil block copolymers as a new architecture for OMIECs. Incorporating PEG and PLLA coils can enhance device performance beyond the homopolymer. The figure‐of‐merit depends uniquely on coil length.
Junfu Tian, Wentao Shan, Rachael Found, Paola Mantegazza, Francesco Leoni, Andreas W. Erhardt, Yuyun Yao, Matus Stredansky, Arianna Magni, Adam Marks, Elena Chulanova, Zeinab Hamid, Yueying Huang, Wanpeng Lu, Xian'e Li, Baopu Zhang, Qingpei Wan, Christina Kousseff, Matilde Concilio, Ruth Theresia Arwani, Caroline A. Ross, Sahika Inal, Giovanni Costantini, Iain McCulloch   +23 more
wiley   +1 more source

Design, Modeling and Synthesis of 1,2,3-Triazole-Linked Nucleoside-Amino Acid Conjugates as Potential Antibacterial Agents

Molecules, 2017
Copper-catalyzed azide-alkyne cycloadditions (CuAAC or click chemistry) are convenient methods to easily couple various pharmacophores or bioactive molecules.
Sarah N. Malkowski, Carolyn F. Dishuck, Gene G. Lamanilao, Carter P. Embry, Christopher S. Grubb, Mauricio Cafiero, Larryn W. Peterson   +6 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

Development of Novel Immobilized Copper–Ligand Complex for Click Chemistry of Biomolecules

Molecules
Copper-catalyzed azide–alkyne cycloaddition click (CuAAC) reaction is widely used to synthesize drug candidates and other biomolecule classes. Homogeneous catalysts, which consist of copper coordinated to a ligand framework, have been optimized for high ...
Rene Kandler, Yomal Benaragama, Manoranjan Bera, Caroline Wang, Rasheda Aktar Samiha, W. M. C. Sameera, Samir Das, Arundhati Nag   +7 more
doaj   +1 more source

In Situ Bioorthogonal Synthesis of PROTACs via Dual‐Responsive Cleavage for Synergistic Photo‐Immunotherapy

Advanced Science, EarlyView.
A bioactive self‐delivering SNAP‐TAC platform responds to tumor‐associated cathepsin B and glutathione, enabling in situ bioorthogonal synthesis of a BRD4‐degrading proteolysis‐targeting chimera within the tumor microenvironment. The resulting BRD4 degradation and PD‐L1 downregulation synergize with photodynamic therapy‐induced immunogenic cell death ...
Shiqin Jian, Jiasha Wu, Fusheng Xu, Yan Zuo, Huaxing Shen, Rui Ji, Luyi Wang, Na Li, Yanting Sun, Yongsheng Yu, Yejiao Shi, Honggang Hu, Feng Xu, Dan Huang, Xiaochun Hu   +14 more
wiley   +1 more source