Results 41 to 50 of about 5,203 (175)

6,7-Dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline amides and corresponding ester isosteres as multidrug resistance reversers

Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Aiming to deepen the structure–activity relationships of the two P-glycoprotein (P-gp) modulators elacridar and tariquidar, a new series of amide and ester derivatives carrying a 6,7-dimethoxy-2-phenethyl-1,2,3,4-tetrahydroisoquinoline scaffold linked to
Laura Braconi, Gianluca Bartolucci, Marialessandra Contino, Niccolò Chiaramonte, Roberta Giampietro, Dina Manetti, Maria Grazia Perrone, Maria Novella Romanelli, Nicola Antonio Colabufo, Chiara Riganti, Silvia Dei, Elisabetta Teodori   +11 more
doaj   +1 more source

Catalytic asymmetric umpolung reaction of imines to synthesize isoindolinones and tetrahydroisoquinolines

Green Synthesis and Catalysis, 2021
Isoindolinone- and tetrahydroisoquinoline-based cyclic scaffolds comprise the key, structural feature of a wide range of biologically active molecules.
Ze-Dong Mou, Xia Zhang, Dawen Niu
doaj   +1 more source

Retro‐Hetero‐Michael Addition Strategies in Organic Synthesis

European Journal of Organic Chemistry, EarlyView.
In this review, synthetic approaches to carbo‐ and heterocyclic compounds, including natural products, published in the last 15 years (2011–2025) which have either relied upon or included a retro‐hetero‐Michael addition step at any stage are discussed.
Dina Scarpi, Ernesto G. Occhiato
wiley   +1 more source

Design, synthesis and activity evaluation of tetrahydroisoquinoline‐based programmed cell death ligand 1 inhibitors

Smart Molecules, EarlyView.
Based on a 3D‐quantitative structure‐activity relationship pharmacophore model, structural optimization of Y6 yielded Y7f. Mechanistic studies revealed that Y7f acted as a programmed death receptor 1/programmed cell death ligand 1 (PD‐L1) interaction inhibitor by inducing PD‐L1 dimerization. Y7f restored T‐cell function.
Menglin Yu, Sen Cai, Yanyan Pan, Heshuang Wang, Fengwu Zhang, Aiyu Ma, Shixuan Lv, Xiuhan Guo, Shisheng Wang, Qiling Song, Chunyan Ma, Shuai Wang, Li Zhang, Jian Wang, Qingwei Meng, Yueqing Li   +15 more
wiley   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Synthesis of C3/C1-Substituted Tetrahydroisoquinolines

Molecules, 2015
A broad biological screening of the natural alkaloid N-methylisosalsoline (2) extracted from Hammada scoparia leaves against a panel of human and parasitic proteases revealed an interesting activity profile of 2 towards human 20S proteasome. This outcome
Mohamed Mihoubi, Nicola Micale, Angela Scala, Raoudha Mezghani Jarraya, Amira Bouaziz, Tanja Schirmeister, Francesco Risitano, Anna Piperno, Giovanni Grassi   +8 more
doaj   +1 more source

Number and Position of Methoxy Substituents Govern Photophysics and Visible‐Light Photocatalysis in Earth‐Abundant Cu(I) Complexes

ChemSusChem, Volume 19, Issue 16, 27 August 2026.
The number and position of methoxy substituents provide a versatile molecular toolbox for tuning the photophysics and visible‐light photocatalytic performance of heteroleptic Cu(I) photosensitizers. Earth‐abundant Cu(I) photosensitizers are promising systems for visible‐light‐driven photocatalysis, but further design guidelines are required to relate ...
Kurt J. Haseloff, Max Wolf, Katharina Rediger, Christian Kleeberg, Maria Wächtler, Stefanie Tschierlei, Michael Karnahl   +6 more
wiley   +1 more source

The One‐Step Synthesis of Biologically Active Isochromans from Lignin‐Derived Aromatic Monomers in Tunable Deep Eutectic Solvents

Chemistry – A European Journal, Volume 32, Issue 30, 13 August 2026.
A straightforward one‐step protocol enables the synthesis of bio‐based and biologically active isochromans through the Oxa‐Pictet cyclization involving diverse aldehydes, including vanillin in combination with lignin‐derivable homovanillyl alcohol, a prominent aromatic platform chemical obtainable via diol‐assisted fractionation of lignocellulose ...
Anjali Kottayi, Anastasiia M. Afanasenko, Antonio A. Castillo‐Garcia, Walid A. M. Elgaher, Jörg Haupenthal, Anna K. H. Hirsch, Katalin Barta   +6 more
wiley   +1 more source

3D Liver Fibrosis Models in Lab: A Novel Modality for Drug Screening

Pharmacology Research &Perspectives, Volume 14, Issue 4, August 2026.
ABSTRACT Liver fibrosis is the common consequence of liver injury caused by a variety of chronic liver disorders. This condition leads to the development of more severe complications, particularly cirrhosis and hepatocellular carcinoma. Despite abundant studies, the fundamental cell and molecular mechanisms of liver fibrosis are still unknown.
Hani Keshavarz Alikhani, Fatemeh Majidi, Mahsa Ghasemzad, Anastasia Shpichka, Anastasia Nestorova, Zahra Hendi, Elham Rismani, Daria Kuznetsova, Peter Timashev, Massoud Vosough, Abbas Piryaei   +10 more
wiley   +1 more source

Crystal structure of 1-(1-chloroethyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolinium chloride

Acta Crystallographica Section E: Crystallographic Communications
1-(1-Chloroethyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline was synthesized through the reaction of homoveratrylamine with racemic lactic acid. The formation of two enantiomers, RR and SS, was detected by performing X-ray diffraction analysis on their
Ziroat E. Urunbaeva, Kambarali K. Turgunov, Abdusalom Sh. Saidov, Valentina I. Vinogradova   +3 more
doaj   +1 more source