Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acs.jafc.2c05223 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
A patent review of von Hippel-Lindau (vhl)-recruiting chemical matter: E3 ligase ligands for PROTACs and targeted protein degradation (2019-present).
Expert Opin Ther Pat
January 2025
Centre for Targeted Protein Degradation, School of Life Sciences, University of Dundee, Dundee, UK.
Introduction: The von Hippel-Lindau (VHL) E3 ubiquitin ligase has seen extensive research due to its involvement in the ubiquitin proteasome system and role as a tumor suppressor within the hypoxia signaling pathway. VHL has become an attractive target for proteolysis targeting chimeras (PROTACs), bifunctional molecules that can induce degradation of neo-substrate proteins. The development of VHL inhibitors and PROTACs has seen rapid development since disclosure of the first non-peptidic VHL ligand (2012).
View Article and Find Full Text PDFSmall molecule ATM inhibitors as potential cancer therapy: a patent review (2003-present).
Expert Opin Ther Pat
January 2025
P. Hertsen Moscow Oncology Research Institute, Moscow, Russian Federation.
Introduction: The ataxia telangiectasia mutated kinase (ATM) is key in coordinating the DDR signaling network essential for responding to double-strand breaks (DSBs). Several ATM inhibitors are being investigated for potential anticancer treatment in clinical trials.
Areas Covered: This review aims to provide a comprehensive overview of patents and patent applications since 2003, with a particular focus on the structural properties, activity and efficacy of the claimed ATM kinase small-molecule inhibitors.
Physicochemical and Biological Evaluation of gem-Difluorinated Saturated Oxygen Heterocycles as Bioisosteres for Drug Discovery.
Chemistry
December 2024
Enamine Ltd., Winston Churchill Street 78, 02094, Kyїv, Ukraine.
A comprehensive study on the physicochemical properties of gem-fluorinated O-heterocyclic substituents is reported. Systematic additive effects of introducing O- and gem-CF group introduction on acidic properties (pK) of the corresponding carboxylic acids/protonated primary amines were demonstrated. The impact of the O/CF moieties on lipophilicity (LogP) was found to be complex; significant mutual influence of the corresponding polar moieties governed the compound's overall properties in this case.
View Article and Find Full Text PDFCopper-Mediated -CF(OCF)(CFH) Transfer to Organic Electrophiles.
ACS Org Inorg Au
December 2024
Department of Chemistry and Biomolecular Sciences and Centre for Catalysis Research and Innovation, University of Ottawa, 30 Marie Curie, Ottawa, Ontario K1N 6N5, Canada.
The integration of fluorine into medicinal compounds has become a widely used strategy to improve the biochemical and therapeutic properties of drugs. Inclusion of -CFH and -OCF fluoroalkyl groups has garnered attention due to their bioisosteric properties, enhanced lipophilicity, and potential hydrogen-bonding capability in bioactive substances. In this study, we prepared a series of stable Cu[CF(OCF)(CFH)]L complexes by insertion of commercially available perfluoro(methyl vinyl ether), CF=CF(OCF), into Cu-H bonds derived from Stryker's reagent, [CuH(PPh)], using ancillary ligands L.
View Article and Find Full Text PDFCircumventing Imatinib resistance in CML: Novel Telmisartan-based cell death modulators with improved activity and stability.
Eur J Med Chem
February 2025
Department of Internal Medicine V, Hematology and Oncology, Tyrolean Cancer Research Institute (TKFI), Comprehensive Cancer Center Innsbruck (CCCI), Medical University of Innsbruck, Anichstrasse 35, 6020 Innsbruck, Austria. Electronic address:
Drug resistance presents a significant challenge in cancer therapy, which has led to intensive research in resistance mechanisms and new therapeutic strategies. In chronic myeloid leukemia (CML), the introduction of Imatinib, the first tyrosine kinase inhibitor (TKI), drastically changed the outcome for patients. However, complete remission still cannot be achieved in a large number of patients in the long term.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!