Results 161 to 170 of about 37,292 (264)
A General Strategy for the Synthesis of Jerangolids Enabled by π‐allyl Stille Coupling
A general strategy for the synthesis of jerangolids is established, featuring a late‐stage π‐allyl Stille coupling of two advanced, highly customizable building blocks to form the skipped diene core. The approach provides access to all naturally occurring jerangolids, including jerangolid H, whose configuration is confirmed by NMR analysis.
Janick Schug +2 more
wiley +1 more source
Expedient Discovery of a Metallaphotoredox Cyanomethylation for Synthesizing α‐Aryl Nitriles
A metallaphotoredox cyanomethylation reaction has been developed for the synthesis of valuable α‐aryl nitrile intermediates. The methodology was successfully applied to diverse medicinally‐relevant substrates, providing an expedient route to anti‐cancer Senexin compounds, while also removing the need for toxic cyanide reagents. The mechanism was probed
Gemma C. Cook +6 more
wiley +1 more source
Synthesis of Novel C‐Acyl‐Glycosyl Sulfonamides via Pd‐Catalyzed Carbonylative Coupling
A Pd‐catalyzed carbonylative coupling of 1‐iodo‐glycals with diverse sulfonamides using Mo(CO)6 enables efficient access to C‐acyl‐glycosyl sulfonamides.This robust and versatile strategy delivers novel glycoside derivatives in good to excellent yields, highlighting their potential for drug discovery.
João A. F. Silva +5 more
wiley +1 more source
Protein-Protein Interaction Stabilizers from MD Simulation-Derived Pharmacophores. [PDF]
Ibrahim M, Zacharias M.
europepmc +1 more source
Screening a lysine‐targeting covalent fragment library against challenging protein targets revealed suitable warheads and characterized binding sites for the development of targeted covalent ligands. Covalent fragment screening has become an established strategy for identifying targetable amino acid residues or viable chemical starting points against ...
Noémi Csorba +18 more
wiley +1 more source
Pharmacophore-Based QSAR Model of Multi Scaffolds as NAMPT Inhibitors & Scaffold Diversity Analysis. [PDF]
Lee S, Zheng M, Kim K, Chun KH.
europepmc +1 more source
Probing 3‐Amino‐2H‐Azaindazoles as Allosteric Inhibitors of the Protein Tyrosine Phosphatase SHP2
A palladium‐catalyzed domino reaction facilitated the discovery and rapid synthesis of selective, potent 3‐amino‐2H‐azaindazole derivatives serving as allosteric inhibitors of SHP2. Structural analysis via co‐crystallography confirmed binding at the allosteric site, thereby stabilizing the autoinhibited SHP2 conformation, qualifying this scaffold as a ...
Machoud Amoussa +20 more
wiley +1 more source
CReM-pharm: de novo 3D pharmacophore-based design with synthetic accessibility awareness. [PDF]
Denzler A +3 more
europepmc +1 more source
Can Chen,1,2,* Ting Wang,1,3,* Fengbo Wu,1,* Wei Huang,4 Gu He,1 Liang Ouyang,1 Mingli Xiang,1 Cheng Peng,4 Qinglin Jiang1,2 1State Key Laboratory of Biotherapy and Department of Pharmacy, West China Hospital, Sichuan University, Chengdu, 2College of ...
Huang W +8 more
core
Herein, an organocatalytic asymmetric synthesis of dihydroquinoline/hydantoin hybrids is described. The synthetic protocol involves a tandem reaction comprising a phosphoric acid–catalyzed initial Povarov dimerization of in situ generated imine/enamine mixtures under tautomeric equilibrium, followed by a Urech–Read reaction of the 1,2‐dihydroquinoline ...
Zuriñe Serna‐Burgos +5 more
wiley +1 more source

