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15 Results Found

  • Article
  • Open Access
1 Citations
1,594 Views
21 Pages

Disubstituted Meldrum’s Acid: Another Scaffold with SuFEx-like Reactivity

  • Baoqi Chen,
  • Zhenguo Wang,
  • Xiaole Peng,
  • Jijun Xie,
  • Zhixiu Sun and
  • Le Li

29 August 2025

Sulfur Fluoride Exchange (SuFEx) chemistry represents an emerging class of click reactions that has found broad applications in drug discovery and materials science. Traditionally, SuFEx reactivity has been regarded as the exclusive privilege of sulf...

  • Article
  • Open Access
5 Citations
4,936 Views
10 Pages

7 January 2023

A practical and efficient Suzuki coupling of phenols has been developed by using trans-NiCl(o-Tol)(PCy3)2/2PCy3 as a catalyst in the presence of tosyl fluoride as an activator. The key for the direct use of phenols lies in the compatibility of the ni...

  • Article
  • Open Access
214 Views
14 Pages

Structure-Aided Design of a LuxR-Type Quorum Sensing SuFEx-Based Potential Inhibitor: Covalent or Competitive Inhibition?

  • Laurent Soulère,
  • Sylvie Reverchon,
  • Jessica Baude,
  • Emmanuel Chefdeville,
  • Antoine Vauchez,
  • Yves Queneau and
  • William Nasser

14 February 2026

New N-benzoyl-l-homoserine lactone derivatives bearing a meta-fluorosulfonyl or a meta-methylsulfonyl group have been designed, synthesized and evaluated as quorum sensing (QS) inhibitors. Docking simulations involving the structure of several target...

  • Short Note
  • Open Access
1 Citations
2,695 Views
6 Pages

2-(4-(Fluorosulfonyloxy)phenyl)benzoxazole

  • Nadezhda V. Danilenko,
  • Mariia O. Lutsuk,
  • Svetlana E. Patlasova,
  • Elena I. Korotkova and
  • Andrei I. Khlebnikov

27 November 2023

New 2-(4-(fluorosulfonyloxy)phenyl)benzoxazole (2) was synthesized through the SuFEx click reaction in a two-chamber reactor. The effect of silylation on the yield of the target compound was investigated. The fluorescent properties of compound 2 were...

  • Short Note
  • Open Access
1,246 Views
4 Pages

4-(Benzoxazol-2-yl)phenyl 3-((3-Chloro-1,4-Naphthoquinon-2-yl)amino)phenyl Sulfate

  • Nadezhda V. Danilenko,
  • Mariia O. Lutsuk and
  • Andrei I. Khlebnikov

5 December 2024

New 4-(benzoxazol-2-yl)phenyl 3-((3-chloro-1,4-naphthoquinon-2-yl)amino)phenyl sulfate was synthesized via the SuFEx click reaction between fluorosulfate-containing 1,4-naphthoquinone and 2-(4-hydroxyphenyl)benzoxazole. 1,8-Diazabicyclo[5.4.0]undec-7...

  • Short Note
  • Open Access
5 Citations
2,866 Views
5 Pages

2-(2-(Fluorosulfonyloxy)phenyl)benzoxazole

  • Nadezhda V. Danilenko,
  • Vladimir I. Shmalyuk and
  • Andrei I. Khlebnikov

2 July 2021

The fluorosulfate derivatives of benzoxazole attract attention since benzoxazole-based compounds have a wide range of biological activities, and the ability of the –SO2F group to react with various functional groups makes it possible to synthesize va...

  • Article
  • Open Access
1,201 Views
19 Pages

Luminescent Properties and Cytotoxic Activity of 2-phenylbenzoxazole Fluorosulfate Derivatives

  • Nadezhda V. Danilenko,
  • Mariia O. Lutsuk,
  • Alexey A. Ryadun,
  • Dmitry I. Pavlov,
  • Evgenii V. Plotnikov,
  • Daria D. Eskova,
  • Yulia D. Klimenko,
  • Andrei S. Potapov and
  • Andrei I. Khlebnikov

The synthesis of 2-phenylbenzoxazole fluorosulfate derivatives was carried out using the SuFEx reaction. To study the anticancer properties of the obtained compounds, the cell lines PC-3 (obtained from prostate adenocarcinoma), BT-474, and MCF-7 (bot...

  • Article
  • Open Access
3 Citations
3,170 Views
25 Pages

Synthesis of New 1,4-Naphthoquinone Fluorosulfate Derivatives and the Study of Their Biological and Electrochemical Properties

  • Natalia V. Aseeva,
  • Nadezhda V. Danilenko,
  • Evgenii V. Plotnikov,
  • Elena I. Korotkova,
  • Olga I. Lipskikh,
  • Anna N. Solomonenko,
  • Alina V. Erkovich,
  • Daria D. Eskova and
  • Andrei I. Khlebnikov

14 November 2024

This study presents the synthesis of new fluorosulfate derivatives of 1,4-naphthoquinone by the SuFEx reaction. Anticancer properties of obtained compounds were studied on PC-3 (prostate adenocarcinoma), SKOV-3 (ovarian cancer), MCF-7 (breast cancer)...

  • Article
  • Open Access
5 Citations
3,706 Views
15 Pages

28 August 2021

Novel polymeric MacMillan catalysts were prepared from modified chiral imidazolidin-4-one monomers via sulfur(VI) fluoride exchange chemistry. The resulting polysulfates containing chiral imidazolidin-4-one units could be employed as polymeric organo...

  • Article
  • Open Access
15 Citations
4,959 Views
14 Pages

Sulfur(VI) Fluoride Exchange (SuFEx)-Mediated Synthesis of the Chitosan-PEG Conjugate and Its Supramolecular Hydrogels for Protein Delivery

  • Kyoung-Je Jang,
  • Woong-Sup Lee,
  • Sangbae Park,
  • Jinsub Han,
  • Jae Eun Kim,
  • B. Moon Kim and
  • Jong Hoon Chung

27 January 2021

Supramolecular hydrogels are considered promising drug carriers in the tissue engineering field due to their versatile nature. Chitosan hydrogels without chemical cross-linkers have low cytotoxicity and good delivery capacity; however, they have lowe...

  • Abstract
  • Open Access
1 Citations
1,584 Views
2 Pages

Sulfur [18F]Fluoride Exchange Reaction Enables Rapid Access to 18F-Labeled PET Tracers

  • Austin Craig,
  • Jürgen Kogler,
  • Fabian Krutzek,
  • Florian Brandt,
  • Markus Laube,
  • Martin Ullrich,
  • Cornelius Kurt Donat,
  • Klaus Kopka and
  • Sven Stadlbauer

16 November 2022

Efficient 18F-fluorination procedures for the production of radiopharmaceuticals are urgently needed to satisfy the increasing demand for clinical diagnostics using positron emission tomography (PET). However, the development of PET tracers is often...

  • Article
  • Open Access
9 Citations
3,718 Views
18 Pages

Preparation of 18F-Labeled Tracers Targeting Fibroblast Activation Protein via Sulfur [18F]Fluoride Exchange Reaction

  • Austin Craig,
  • Jürgen Kogler,
  • Markus Laube,
  • Martin Ullrich,
  • Cornelius K. Donat,
  • Robert Wodtke,
  • Klaus Kopka and
  • Sven Stadlbauer

Early detection and treatment of cancers can significantly increase patient prognosis and enhance the quality of life of affected patients. The emerging significance of the tumor microenvironment (TME) as a new frontier for cancer diagnosis and thera...

  • Communication
  • Open Access
18 Citations
3,660 Views
9 Pages

A major obstacle to the therapeutic application of an aptamer is its susceptibility to nuclease digestion. Here, we confirmed the acquisition of relative nuclease resistance of a DNA-type thrombin binding aptamer with a warhead (TBA3) by covalent bin...

  • Article
  • Open Access
5 Citations
6,015 Views
17 Pages

Activation-Free Sulfonyl Fluoride Probes for Fragment Screening

  • László Petri,
  • Péter Ábrányi-Balogh,
  • Noémi Csorba,
  • Aaron Keeley,
  • József Simon,
  • Ivan Ranđelović,
  • József Tóvári,
  • Gitta Schlosser,
  • Dániel Szabó and
  • György M. Keserű
  • + 1 author

29 March 2023

SuFEx chemistry is based on the unique reactivity of the sulfonyl fluoride group with a range of nucleophiles. Accordingly, sulfonyl fluorides label multiple nucleophilic amino acid residues, making these reagents popular in both chemical biology and...

  • Review
  • Open Access
3 Citations
3,317 Views
17 Pages

26 September 2024

Background: The incorporation of radionuclides into peptides and larger biomolecules requires efficient and sometimes biorthogonal reaction conditions, to which click chemistry provides a convenient approach. Methods: Traditionally, click-based radio...