ArticleJournal of medicinal chemistry2013
Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation.
Article in Journal of medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
17 citing papers in PubMed, 42 citations in OpenAlex.
- Molecular Imaging of Pancreatic Duct Adenocarcinoma Using [Molecular imaging and biology · 2026Article
- Discovery of Potent and Selective CB2 Agonists Utilizing a Function-Based Computational Screening Protocol.ACS chemical neuroscience · 2023Article
- Article
- The Role of Cannabinoids in Bone Metabolism: A New Perspective for Bone Disorders.International journal of molecular sciences · 2021Review
- Tricyclic Pyrazole-Based Compounds as Useful Scaffolds for Cannabinoid CBMolecules (Basel, Switzerland) · 2021Review
- Xie2-64, a novel CBNeuropharmacology · 2020Article
- Review
- PSTP-3,5-Me Inhibits Osteoclast Differentiation and Bone Resorption.Molecules (Basel, Switzerland) · 2019Article
- Prediction of Orthosteric and Allosteric Regulations on Cannabinoid Receptors Using Supervised Machine Learning Classifiers.Molecular pharmaceutics · 2019Article
- Targeted inhibition of the type 2 cannabinoid receptor is a novel approach to reduce renal fibrosis.Kidney international · 2018Article
- The tamoxifen derivative ridaifen-B is a high affinity selective CBToxicology and applied pharmacology · 2018Article
- Multi-Functional Diarylurea Small Molecule Inhibitors of TRPV1 with Therapeutic Potential for Neuroinflammation.The AAPS journal · 2016Article
- Difference and Influence of Inactive and Active States of Cannabinoid Receptor Subtype CB2: From Conformation to Drug Discovery.Journal of chemical information and modeling · 2016Article
- Discovery of novel INK4C small-molecule inhibitors to promote human and murine hematopoietic stem cell ex vivo expansion.Scientific reports · 2015Article
- Ligand biological activity predictions using fingerprint-based artificial neural networks (FANN-QSAR).Methods in molecular biology (Clifton, N.J.) · 2015Article
- Modeling, molecular dynamics simulation, and mutation validation for structure of cannabinoid receptor 2 based on known crystal structures of GPCRs.Journal of chemical information and modeling · 2014Article
- Recent advances in antimultiple myeloma drug development.Pharmaceutical patent analyst · 2014Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
Cannabinoid receptors have gained increasing attention as drug targets for developing potential therapeutic ligands. Here, we report the discovery and optimization of triaryl sulfonamides as a novel series possessing significant CB2 receptor affinity and selectivity. Four sets of triaryl ligands were designed and synthesized for further structural modifications and led to the identification of eight compounds as potent and selective CB2 inverse agonists with high binding affinity (CB2K(i) < 10 nM). Especially, compound 57 exhibited the strongest binding affinity on the CB2 receptor (CB2K(i) of 0.5 nM) and the best selectivity over the CB1 receptor (selectivity index of 2594). Importantly, 57 also showed potent inhibitory activity on osteoclast formation, and it was confirmed by a cell viability assay that the inhibition effects were not derived from the cytotoxicity. Finally, 3D QSAR studies confirmed our SAR findings that three bulky groups play an important role for CB2 receptor binding affinity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.