High throughput screening of a library based on kinase inhibitor scaffolds against Mycobacterium tuberculosis H37Rv

RC Reynolds, S Ananthan, E Faaleolea, JV Hobrath… - Tuberculosis, 2012 - Elsevier
Kinase targets are being pursued in a variety of diseases beyond cancer, including immune
and metabolic as well as viral, parasitic, fungal and bacterial. In particular, there is a …

Novel N-(3-carboxyl-9-benzyl-β-carboline-1-yl) ethylamino acids: synthesis, anti-tumor evaluation, intercalating determination, 3D QSAR analysis and docking …

J Wu, M Zhao, K Qian, KH Lee… - European journal of …, 2009 - Elsevier
Sixteen novel N-(3-carboxyl-9-benzyl-β-carboline-1-yl) ethylamino acids (6a–p) were
synthesized as intercalating lead compounds. In the in vitro cytotoxic assay their IC50 values …

[HTML][HTML] New NADPH Oxidase 2 Inhibitors Display Potent Activity against Oxidative Stress by Targeting p22phox-p47phox Interactions

AV Treuer, M Faúndez, R Ebensperger, E Hovelmeyer… - Antioxidants, 2023 - mdpi.com
NADPH oxidase (NOX2) is responsible for reactive oxygen species (ROS) production in
neutrophils and has been recognized as a key mediator in inflammatory and cardiovascular …

A class of oral N-[(1S, 3S)-1-methyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carbonyl]-N′-(amino-acid-acyl) hydrazine: Discovery, synthesis, in vitro anti-platelet …

K Yao, M Zhao, X Zhang, Y Wang, L Li, M Zheng… - European journal of …, 2011 - Elsevier
The in vivo anti-thrombotic activities of amino acid modified tetrahydro-β-carbolines
depended upon the proximity of the side chain of the amino acid residue to the carboline …

Discovery of new JNK3 inhibitory chemotypes via QSAR-Guided selection of docking-based pharmacophores and comparison with other structure-based …

GO Tuffaha, MH Ma'mon, MO Taha - Journal of Molecular Graphics and …, 2019 - Elsevier
The kinase c-Jun N-terminal Kinase 3 (JNK3) plays an important role in neurodegenerative
diseases. JNK3 inhibitors have shown promising results in treating Alzheimer's and …

A class of novel Schiff's bases: Synthesis, therapeutic action for chronic pain, anti-inflammation and 3D QSAR analysis

Y Zhou, M Zhao, Y Wu, C Li, J Wu, M Zheng… - Bioorganic & medicinal …, 2010 - Elsevier
To discover analgesics for treating chronic pain 17 novel Schiff's bases, N, N′-(Z-allylidene-
1, 3-diyl) bisamino acid methyl esters were prepared from 1, 1, 3, 3,-tetramethoxypropane …

A class of novel carboline intercalators: Their synthesis, in vitro anti-proliferation, in vivo anti-tumor action, and 3D QSAR analysis

J Wu, C Li, M Zhao, W Wang, Y Wang… - Bioorganic & medicinal …, 2010 - Elsevier
Based on DOCK scores 18 N-(3-benzyloxycarbonylcarboline-1-yl) ethylamino acid
benzylesters (6a–r) were synthesized as anti-tumor agents. Their IC50 values against five …

Quantitative structure–activity relationship studies on 1-aryl-tetrahydroisoquinoline analogs as active anti-HIV agents

K Chen, H **e, Z Li, J Gao - Bioorganic & medicinal chemistry letters, 2008 - Elsevier
Predictive quantitative structure–activity relationship analysis was developed for a diverse
series of recently synthesized 1-aryl-tetrahydroisoquinoline analogs with anti-HIV activities …

(3S)-N-(l-Aminoacyl)-1, 2, 3, 4-tetrahydroisoquinolines, a class of novel antithrombotic agents: Synthesis, bioassay, 3D QSAR, and ADME analysis

M Zheng, X Zhang, M Zhao, HW Chang… - Bioorganic & medicinal …, 2008 - Elsevier
To increase antithrombotic activity, 3S-tetrahydroisoquinoline-3-carboxylic acid (1) was
modified with natural amino acids to form 19 novel dipeptide analogs, 3S …