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.
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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.
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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
Chromene Derivatives as Selective TERRA G-Quadruplex RNA Binders with Antiproliferative Properties
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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