Synergistic exploration of antimicrobial potency, cytotoxicity, and molecular mechanisms: A tripartite investigation integrating in vitro, in vivo, and in silico approaches for pyrimidine‐based metal (II) complexes
Sign Up to like & getrecommendations! Published in 2024 at "Applied Organometallic Chemistry"
DOI: 10.1002/aoc.7521
Abstract: We synthesized and characterized bioactive metal (II) complexes from a pyrimidine‐based Schiff base ligand, 4‐[2‐(4‐chlorobenzylidene) hydrazinyl]‐7H‐pyrrolo[2,3‐d]pyrimidine. Through thorough elemental analysis and various physicochemical techniques, we characterized both the ligand and its Zn(II), Cd(II), and Hg(II)… read more here.
Keywords: ligand; metal; pyrimidine based; metal complexes ... See more keywords
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
Discovery of Novel Pyrimidine-Based Derivatives as Nav1.2 Inhibitors with Efficacy in Mouse Models of Epilepsy.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c00861
Abstract: Dysfunction of voltage-gated sodium channel Nav1.2 causes various epileptic disorders, and inhibition of the channel has emerged as an attractive therapeutic strategy. However, currently available Nav1.2 inhibitors exhibit low potency and limited structural diversity. In… read more here.
Keywords: nav1 inhibitors; pyrimidine based; based derivatives; discovery novel ... See more keywords
Pyrazolo[1,5-a]pyrimidine-Based Type-I Photosensitizer as an Efficient Pyroptosis Inducer for Tumor Ablation.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c03075
Abstract: Pyroptosis is a proinflammatory and lytic programmed cell death form, which can promote cytotoxic T lymphocyte (CTL) maturation and tumor infiltration through the release of damage-associated molecular patterns (DAMPs). Therefore, the induction of pyroptosis by… read more here.
Keywords: pyroptosis; pyrazolo pyrimidine; tumor; based type ... See more keywords
Discovery of Potent and Selective Pyrrolo[2,3-d]Pyrimidine-Based Aurora A Inhibitors with Demonstrated Efficacy against Patient-Derived Gastric Cancer Organoids.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.5c01886
Abstract: Aurora A kinase, a key regulator of mitosis, has emerged as a promising therapeutic target for gastric cancer. However, challenges related to selectivity and resistance highlight the urgent need for novel Aurora A inhibitors with… read more here.
Keywords: cancer; pyrrolo pyrimidine; based aurora; gastric cancer ... 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