Design and synthesis of novel quinazolin‐4(1H)‐one derivatives as potent and selective inhibitors targeting AKR1B1
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200577
Abstract: Inhibition of aldose reductase (AKR1B1) is a promising option for the treatment of diabetic complications. However, most of the developed small molecule inhibitors lack selectivity or suffer from low bioactivity. To address this limitation, a… read more here.
Keywords: design synthesis; derivatives potent; quinazolin one; selective inhibitors ... See more keywords
Xylose‐Configured Cyclophellitols as Selective Inhibitors for Glucocerebrosidase
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DOI: 10.1002/cbic.202100396
Abstract: Glucocerebrosidase (GBA), a lysosomal retaining β‐d‐glucosidase, has recently been shown to hydrolyze β‐d‐xylosides and to transxylosylate cholesterol. Genetic defects in GBA cause the lysosomal storage disorder Gaucher disease (GD), and also constitute a risk factor… read more here.
Keywords: xylose configured; gba; cyclophellitols selective; selective inhibitors ... See more keywords
Nucleobase Modified Adefovir (PMEA) Analogues as Potent and Selective Inhibitors of Adenylate Cyclases from Bordetella pertussis and Bacillus anthracis
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DOI: 10.1002/cmdc.201800332
Abstract: A series of 13 acyclic nucleoside phosphonates (ANPs) as bisamidate prodrugs was prepared. Five compounds were found to be non‐cytotoxic and selective inhibitors of Bordetella pertussis adenylate cyclase toxin (ACT) in J774A.1 macrophage cell‐based assays.… read more here.
Keywords: potent selective; adenylate cyclases; bacillus anthracis; bordetella pertussis ... See more keywords
Antiviral lectins: Selective inhibitors of viral entry
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DOI: 10.1016/j.antiviral.2017.03.007
Abstract: Abstract Many natural lectins have been reported to have antiviral activity. As some of these have been put forward as potential development candidates for preventing or treating viral infections, we have set out in this… read more here.
Keywords: reported antiviral; inhibitors viral; antiviral lectins; selective inhibitors ... See more keywords
Structure-based design and synthesis of 2,4-diaminopyrimidines as EGFR L858R/T790M selective inhibitors for NSCLC.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.08.061
Abstract: Mutated epidermal growth factor receptor (EGFR) is a major driver of non-small cell lung cancer (NSCLC). The EGFRT790M secondary mutation has become a leading cause of clinically-acquired resistance to gefitinib and erlotinib. Herein, we present… read more here.
Keywords: design synthesis; selective inhibitors; structure based; structure ... See more keywords
Targeting breast cancer stem cells by novel HDAC3-selective inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.08.069
Abstract: Although histone deacetylase (HDAC) inhibitors have been known to suppress the cancer stem cell (CSC) population in multiple types of cancer cells, it remains unclear which HDAC isoforms and corresponding mechanisms contribute to this anti-CSC… read more here.
Keywords: cancer stem; hdac3 selective; breast cancer; selective inhibitors ... See more keywords
Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111646
Abstract: The immunoproteasome, a specialized form of proteasome, is mainly expressed in lymphocytes and monocytes of jawed vertebrates and responsible for the generation of antigenic peptides for cell-mediated immunity. Overexpression of immunoproteasome have been detected in… read more here.
Keywords: overview recent; inhibitors overview; recent developments; immunoproteasome selective ... See more keywords
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111710
Abstract: Aberrant activation of FMS-like tyrosine receptor kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid leukemia (AML) in 20-30% of patients. In this study we identified a highly selective (phenylethenyl)quinazoline compound family as… read more here.
Keywords: development extreme; discovery development; flt3; extreme selective ... See more keywords
Discovery of imidazopyrrolopyridines derivatives as novel and selective inhibitors of JAK2.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113394
Abstract: Herein, we describe the design, synthesis, and structure-activity relationships of a series of imidazopyrrolopyridines derivatives that selectively inhibit Janus kinase 2 (JAK2). These screening cascades revealed that 6k was a preferred compound, with IC50 values… read more here.
Keywords: imidazopyrrolopyridines derivatives; derivatives novel; discovery imidazopyrrolopyridines; novel selective ... See more keywords
Selective Inhibitors of AlkB Family of Nucleic Acid Demethylases.
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DOI: 10.1021/acs.biochem.9b00774
Abstract: The α-ketoglutarate-dependent (AlkB) superfamily of FeII/2-oxoglutarate (2-OG) -dependent dioxygenases consists of a unique class of nucleic acid repair enzymes which reversibly remove alkyl substituents from nucleobases through oxidative dealkylation. Recent studies have verified the involvement… read more here.
Keywords: family nucleic; alkb family; inhibitors alkb; selective inhibitors ... See more keywords
Selective Inhibitor Design for Kinase Homologs Using Multiobjective Monte Carlo Tree Search
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Chemical Information and Modeling"
DOI: 10.1021/acs.jcim.2c00787
Abstract: Designing highly selective molecules for a drug target protein is a challenging task in drug discovery. This task can be regarded as a multiobjective problem that simultaneously satisfies criteria for various objectives, such as selectivity… read more here.
Keywords: structure; selective inhibitors; structure generator; target protein ... See more keywords