Alkyne‐ and azide‐functionalised cyclophellitol derivatives for selective glucuronidase targeting
Sign Up to like & getrecommendations! Published in 2024 at "European Journal of Organic Chemistry"
DOI: 10.1002/ejoc.202401076
Abstract: Heparanase is an endo‐acting β‐glucuronidase and the only known enzyme responsible for the regulation of heparan sulfate structures in the extracellular matrix. The enzyme is found to be significantly upregulated in aggressive cancer types, aiding… read more here.
Keywords: functionalised cyclophellitol; cyclophellitol derivatives; glucuronidase; derivatives selective ... See more keywords
N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01488
Abstract: In this study, we described a series of N-(pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine derivatives as selective JAK2 (Janus kinase 2) inhibitors. Systematic exploration of the structure-activity relationship though cyclization modification based on previously reported compound 18e led to the… read more here.
Keywords: amine derivatives; tetrahydroisoquinolin amine; kinase; derivatives selective ... See more keywords
Multiparameter Optimization of Naphthyridine Derivatives as Selective α5-GABAA Receptor Negative Allosteric Modulators.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00414
Abstract: The discovery and characterization of novel naphthyridine derivatives with selective α5-GABAAR negative allosteric modulator (NAM) activity are disclosed. Utilizing a scaffold-hopping strategy, fused [6 + 6] bicyclic scaffolds were designed and synthesized. Among these, 1,6-naphthyridinones… read more here.
Keywords: selective gabaa; optimization naphthyridine; derivatives selective; multiparameter optimization ... See more keywords
Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00242
Abstract: The NLRP3 inflammasome is a multiprotein complex that facilitates activation and release of the proinflammatory cytokines interleukin-1β (IL-1β) and IL-18 in response to infection or endogenous stimuli. It can be inappropriately activated by a range… read more here.
Keywords: triazolopyrimidinone derivatives; derivatives selective; optimization triazolopyrimidinone; discovery optimization ... See more keywords
Pyrimidine Derivatives as Selective COX-2 Inhibitors with Anti-Inflammatory and Antioxidant Properties
Sign Up to like & getrecommendations! Published in 2024 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms252011011
Abstract: Pyrimidine derivatives exhibit a wide range of biological activities, including anti-inflammatory properties. The aim of this study was to investigate the effects of tested pyrimidine derivatives on the activity of cyclooxygenase isoenzymes (COX-1 and COX-2),… read more here.
Keywords: pyrimidine derivatives; derivatives selective; antioxidant properties; anti inflammatory ... See more keywords
Chromene Derivatives as Selective TERRA G-Quadruplex RNA Binders with Antiproliferative Properties
Sign Up to like & getrecommendations! Published in 2022 at "Pharmaceuticals"
DOI: 10.3390/ph15050548
Abstract: In mammalian cells, telomerase transcribes telomeres in large G-rich non-coding RNA, known as telomeric repeat-containing RNA (TERRA), which folds into noncanonical nucleic acid secondary structures called G-quadruplexes (G4s). Since TERRA G4 has been shown to… read more here.
Keywords: chromene derivatives; selective terra; derivatives selective; rna ... See more keywords