Readily accessible N‐allyl‐N‐2‐bromoallylamines undergo a tandem lithiation–cyclization cascade to furnish highly substituted 3‐azabicyclo[3.1.0]hexanes. The transformation proceeds without transition metals and delivers products with excellent diastereocontrol across a broad substrate range.
Nuria Cases +5 more
wiley +1 more source
Generation of the Camptothecin Scaffold by a Flavin‐Catalyzed Photooxidative Skeletal Reorganization
The biosynthetic pathway of the anticancer drug precursor camptothecin involves an enigmatic skeletal reorganization from a 6/5/6 tetrahydro‐β‐carboline to a 6/6/5 pyrroloquinoline ring system. Here, we show that this transformation can be achieved by photooxidation with flavin cofactors, such as flavin mononucleotide (FMN) as catalysts.
Shenyu Liu +6 more
wiley +2 more sources
Unspecific Peroxygenase-Based Chemo-Enzymatic Synthesis of Amino Alcohols for Pharmaceutical Preparation. [PDF]
Last S +5 more
europepmc +1 more source
Mechanical Activation of Piezo1 Drives Osteoarthritis Through Kdm5c‐Mediated Epigenetic Silencing
Excessive mechanical stress activates Piezo1, triggering Ca2+‐dependent cytoskeletal forces that deform the nucleus and reduce H3K4me3. Kdm5c demethylates H3K4me3 at Col2a1 and Runx3 promoters. Kdm5c knockout rescues degradation. Repurposed telmisartan directly inhibits Kdm5c, blocking this axis and showing disease‐modifying efficacy in mouse OA models
Tianyou Kan +13 more
wiley +1 more source
Cytochrome P450- and Dehydrogenase-Mediated Regiospecific and Stereoselective Formation of β- and γ-Lactones in Drimane-Type Sesquiterpenoid Biosynthesis. [PDF]
Wu M, Wu J, Janzen DJ, Yin WB, Li SM.
europepmc +1 more source
Untangling Inositol (Pyro)Phosphate Biology Through Emerging Technologies
Inositol (pyro)phosphates represent a vital class of intracellular messengers that govern multiple biological processes. The last decade has experienced a surge of interest in the functions of this class of signaling molecules, primarily due to the introduction of several innovative analytical technologies.
Adolfo Saiardi +5 more
wiley +1 more source
Single Amino Acid-Based Control of Fibril Supramolecular Chirality. [PDF]
Sitton J, Kurouski D.
europepmc +1 more source
Synthesis of 3,5‐Diarylated 4‐Cyano‐2‐nitrophenols via Nitro Rearrangement
A practical synthetic route to 3,5‐diaryl‐4‐cyano‐2‐nitrophenols, a class of unsymmetrically substituted and densely functionalized phenols, is provided. The key transformation is a nitro rearrangement of 4‐cyano‐4‐nitrocyclohexanone derivatives, which were prepared from di(benzylidene)acetones through cyano(nitro)methylation.
Nagatoshi Nishiwaki +3 more
wiley +1 more source
A Novel, Robust, and Isocratic HPLC-UV Method for the Comprehensive Determination of Enantiomeric Impurity (R-Isomer) in Niraparib Drug Substance. [PDF]
Kondaveti PK +3 more
europepmc +1 more source
Flavouring Group Evaluation 82 Revision 2 (FGE.82Rev2): Consideration of epoxides evaluated by JECFA. [PDF]
EFSA Panel on Food Additives and Flavourings (FAF) +22 more
europepmc +1 more source

