Pyrimidine‐Based Fluorescent Probe for Monitoring Mitophagy via Detection of Mitochondrial pH Variation
Sign Up to like & getrecommendations! Published in 2022 at "ChemBioChem"
DOI: 10.1002/cbic.202200217
Abstract: Impaired mitophagy hinders the clearance of damaged mitochondria, inducing pathological states. Knowledge of this phenomenon is key to diagnosing certain diseases and understanding their pathogenesis. Mitophagy involves an acidization process that could serve as an… read more here.
Keywords: variation; mitophagy; detection; based fluorescent ... See more keywords
Design, synthesis and biological evaluation of pyrimidine-based derivatives as VEGFR-2 tyrosine kinase inhibitors.
Sign Up to like & getrecommendations! Published in 2018 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.04.005
Abstract: Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has already become an attractive approach for cancer therapy. In this study, a novel pyrimidine-based… read more here.
Keywords: design synthesis; biological evaluation; evaluation pyrimidine; pyrimidine ... See more keywords
Improvement of cardiomyocyte function by a novel pyrimidine-based CaMKII-inhibitor.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of molecular and cellular cardiology"
DOI: 10.1016/j.yjmcc.2017.12.015
Abstract: OBJECTIVE Pathologically increased activity of Ca2+/calmodulin-dependent protein kinase II (CaMKII) and the associated Ca2+-leak from the sarcoplasmic reticulum are recognized to be important novel pharmacotherapeutic targets in heart failure and cardiac arrhythmias. However, CaMKII-inhibitory compounds… read more here.
Keywords: camkii inhibitor; pyrimidine based; novel pyrimidine; ca2 ... See more keywords
Discovery and Synthesis of a Pyrimidine-Based Aurora Kinase Inhibitor to Reduce Levels of MYC Oncoproteins
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.0c01806
Abstract: The A-type Aurora kinase is upregulated in many human cancers, and it stabilizes MYC-family oncoproteins, which have long been considered an undruggable target. Here, we describe the design and synthesis of a series of pyrimidine-based… read more here.
Keywords: reduce levels; kinase; pyrimidine based; aurora kinase ... See more keywords
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-a]pyrimidine-Based Macrocycles.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00173
Abstract: Serine/threonine kinase 17A (death-associated protein kinase-related apoptosis-inducing protein kinase 1─DRAK1) is a part of the death-associated protein kinase (DAPK) family and belongs to the so-called dark kinome. Thus, the current state of knowledge of the… read more here.
Keywords: threonine kinase; pyrazolo pyrimidine; kinase 17a; kinase ... See more keywords
Design, Synthesis, and Preclinical Evaluation of Fused Pyrimidine-Based Hydroxamates for the Treatment of Hepatocellular Carcinoma.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01465
Abstract: Class I histone deacetylases (HDACs) are highly expressed and/or upregulated in hepatocellular carcinoma (HCC) and are associated with aggressiveness, spread, and increased mortality of HCC. Activation of phosphatidylinositol 3-kinase-Akt-mammalian target of rapamycin (PI3K/Akt/mTOR) signaling pathway… read more here.
Keywords: hepatocellular carcinoma; based hydroxamates; hcc; pyrimidine based ... See more keywords
Trifluorinated Pyrimidine-Based A2B Antagonists: Optimization and Evidences of Stereospecific Recognition.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01340
Abstract: We report the identification of two subsets of fluorinated nonxanthine A2B adenosine receptor antagonists. The novel derivatives explore the effect of fluorination at different positions of two pyrimidine-based scaffolds. The most interesting ligands combine excellent… read more here.
Keywords: antagonists optimization; trifluorinated pyrimidine; pyrimidine; based a2b ... See more keywords
Palladium-catalyzed meta-C-H allylation of arenes: A unique combination of pyrimidine-based template and hexafluoroisopropanol.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.0c05223
Abstract: Controlling remote selectivity and delivering novel functionalities at distal positions in arenes are an important endeavor in contemporary organic synthesis. In this vein, template engineering and mechanistic understanding of new functionalization strategies are essential for… read more here.
Keywords: allylation arenes; template; meta allylation; palladium ... See more keywords
Identification of novel furo[2,3-d]pyrimidine based chalcones as potent anti-breast cancer agents: synthesis, in vitro and in vivo biological evaluation
Sign Up to like & getrecommendations! Published in 2022 at "RSC Advances"
DOI: 10.1039/d2ra00889k
Abstract: Various substituted synthetic chalcones demonstrated potent anti-cancer activities. In the current study a series of novel furo[2,3-d]pyrimidine based chalcones were synthesized as potential anticancer agents. Among the different substituted derivatives, two of the halogen bearing… read more here.
Keywords: novel furo; based chalcones; potent anti; pyrimidine based ... See more keywords
Development of pyrazolo[1,5-a]pyrimidine-based antibacterial agents
Sign Up to like & getrecommendations! Published in 2023 at "Synthetic Communications"
DOI: 10.1080/00397911.2023.2209815
Abstract: Abstract In the present study, a facile method was adopted to efficiently prepare new pyrazolo[1,5-a]pyrimidin-2-amines linked to arene units in good to excellent yields. A mixture of acetophenones and DMF-DMA was heated at 120 oC… read more here.
Keywords: antibacterial activity; based antibacterial; pyrazolo pyrimidine; pyrazolo ... See more keywords
Recent advances in the development of pyrimidine-based CNS agents.
Sign Up to like & getrecommendations! Published in 2022 at "Current drug discovery technologies"
DOI: 10.2174/1570163819666221003094402
Abstract: BACKGROUND In the past few decades, considerable progress has been made in CNS drug discovery, and various new CNS agents have been developed. Pyrimidine is an important scaffold in the area of medicinal chemistry. Recently,… read more here.
Keywords: based cns; development; cns; pyrimidine based ... See more keywords