LAUSR

Kinetic Target‐Guided Synthesis of Small‐Molecule G‐Quadruplex Stabilizers

Sign Up to like & get
recommendations!
0 Published in 2020 at "ChemistryOpen"

DOI: 10.1002/open.202000261

Abstract: Abstract The formation of a G‐quadruplex motif in the promoter region of the c‐MYC protooncogene prevents its expression. Accordingly, G‐quadruplex stabilization by a suitable ligand may be a viable approach for anticancer therapy. In our… read more here.

Keywords: target guided; guided synthesis; molecule; kinetic target ... See more keywords

The emergence of sulfo-click amidation in kinetic target-guided synthesis

Sign Up to like & get
recommendations!
0 Published in 2024 at "Medicinal Chemistry Research"

DOI: 10.1007/s00044-024-03236-w

Abstract: Sulfo-click is a chemoselective and biocompatible reaction between thioacids and sulfonyl azides that forms highly versatile N-acylsulfonamides, interesting bioisosteres of carboxylic acids. This reaction is useful for chemists and biologists and has many applications in… read more here.

Keywords: chemistry; target guided; sulfo click; guided synthesis ... See more keywords

Tailored Bioorthogonal and Bioconjugate Chemistry: A Source of Inspiration for Developing Kinetic Target-Guided Synthesis Strategies.

Sign Up to like & get
recommendations!
0 Published in 2020 at "Bioconjugate chemistry"

DOI: 10.1021/acs.bioconjchem.0c00568

Abstract: Kinetic target-guided synthesis (KTGS) is a promising tool for the discovery of biologically active compounds. It relies on the identification of potent ligands that are covalently assembled by the biological targets themselves from a pool… read more here.

Keywords: guided synthesis; target guided; chemistry; kinetic target ... See more keywords

Going beyond Binary: Rapid Identification of Protein-Protein Interaction Modulators Using a Multifragment Kinetic Target-Guided Synthesis Approach.

Sign Up to like & get
recommendations!
2 Published in 2023 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.3c00108

Abstract: Kinetic target-guided synthesis (KTGS) is a powerful screening approach that enables identification of small molecule modulators for biomolecules. While many KTGS variants have emerged, a majority of the examples suffer from limited throughput and a… read more here.

Keywords: ktgs; guided synthesis; kinetic target; target guided ... See more keywords

Chemoselective seleno-click amidation in kinetic target-guided synthesis.

Sign Up to like & get
recommendations!
0 Published in 2024 at "Chemical communications"

DOI: 10.1039/d4cc04491f

Abstract: Capitalizing on our previous kinetic target-guided synthesis (KTGS) involving the sulfo-click reaction to form N-acylsulfonamide-linked inhibitors in the presence of the protein-protein interaction target Mcl-1, we herein report a seleno-click approach for amide-linked inhibitors of… read more here.

Keywords: target guided; guided synthesis; target; seleno click ... See more keywords