Results 51 to 60 of about 5,203 (175)
Safracin B as a Synthetic Linchpin: From Natural Product to Drug Intermediate and Beyond
Safracin B is employed as a key precursor for the streamlined preparation of cyanosafracin B and safracin A. Careful tuning of the reaction parameters affords these derivatives in high efficiency, and full nuclear magnetic resonance signal assignments are established for the complex safracin frameworks.
Paolo Orlando +5 more
wiley +1 more source
Conformational restriction strategies to increase the activity and selectivity of the STAT5b inhibitor Stafib‐2 are presented. The best conformationally restricted inhibitor Stafib‐2‐CR has threefold higher activity against STAT5b than Stafib‐2. A cell‐permeable prodrug of Stafib‐2‐CR inhibits phosphorylation of STAT5b in cultured human leukemia cells ...
Theresa Münzel +5 more
wiley +1 more source
2-(4-Iodophenyl)-1,2,3,4-tetrahydroisoquinoline-1-carbonitrile
In the title compound, C16H13IN2, the benzene ring of the tetrahydroisoquinoline moiety makes a dihedral angle of 45.02 (9)° with the benzene ring of the 4-iodophenyl fragment.
Yanni Ma +4 more
doaj +1 more source
A new series of structurally rich polyaromatic isonitriles is presented as photoredox catalysts. Their photophysical properties are investigated by UV–Vis absorption and fluorescence measurements, combined with experimental and theoretical studies to evaluate both ground‐ and excited‐state redox properties.
Cristina Martini +9 more
wiley +1 more source
Background: 1,2,3,4-Tetrahydroisoquinolines (THIQs) are common motifs in alkaloids and in medicinal chemistry. Synthetic access to THIQs via the Pomeranz–Fritsch–Bobbit (PFB) methodology using mineral acids for deactivated, electron-poor aromatic systems,
Marco Mottinelli +2 more
doaj +1 more source
4-[(2,4-Dimethylthiazol-5-yl)methyl]-4-hydroxy-2-methylisoquinoline-1,3(2H,4H)-dione
In the title isoquinolinedione derivative, C16H16N2O3S, the piperidine ring in the tetrahydroisoquinoline ring system adopts a distorted envelope conformation.
Hoong-Kun Fun +3 more
doaj +1 more source
Discovery of a Potent Fluorescence Polarization Probe for Identifying USP1 Allosteric Inhibitors
This study presents the first ubiquitin‐specific protease 1 (USP1) allosteric fluoroprobe and fluorescence polarization assay, enabling the differentiation of allosteric and catalytic site inhibitors. Further, a novel class of tetrahydroisoquinoline‐based USP1 inhibitors is designed, with compound 14a (USP1 IC50 = 29.9 nM) showing strong selectivity ...
Jiawei Cheng +12 more
wiley +1 more source
Palladium-Catalyzed α-Arylation of Esters: Synthesis of the Tetrahydroisoquinoline Ring
The palladium-catalyzed cross-coupling reaction used for carbon–carbon bond formation is one of the most commonly applied reactions in modern organic synthesis.
Georgeta Serban, Faïza Diaba
doaj +1 more source
4-[(2,5-Dimethyl-1,3-thiazol-4-yl)methyl]-4-hydroxy-2-methylisoquinoline-1,3(2H,4H)-dione
In the title isoquinolinedione compound, C16H16N2O3S, the piperidine ring in the tetrahydroisoquinoline ring system adopts a half-boat conformation. The essentially planar thiazole ring [maximum deviation = 0.007 (2) Å] makes
Hoong-Kun Fun +3 more
doaj +1 more source
Nucleophilic trapping of iminium salts generated via oxidative functionalisation of tertiary amines is well established with stabilised carbon nucleophiles.
Joshua P. Barham +2 more
doaj +1 more source

