Search Results - "Roh, Eun Joo"
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AKF-D52, a Synthetic Phenoxypyrimidine-Urea Derivative, Triggers Extrinsic/Intrinsic Apoptosis and Cytoprotective Autophagy in Human Non-Small Cell Lung Cancer Cells
Published in Cancers (22-11-2021)“…Previously, we discovered that 1-(3,5-dimethoxyphenyl)-3-(4-(3-methoxyphenoxy)-2-((4-morpholinophenyl)amino)pyrimidin-5-yl)urea (AKF-D52), a synthetic…”
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MRS2500 [2-iodo-N6-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate], a potent, selective, and stable antagonist of the platelet P2Y1 receptor with strong antithrombotic activity in mice
Published in The Journal of pharmacology and experimental therapeutics (01-02-2006)“…The platelet P2Y(1) ADP receptor is an attractive target for new antiplatelet drugs. However, because of the lack of strong and stable antagonists, only a few…”
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3
Death‐associated protein kinase (DAPK) family modulators: Current and future therapeutic outcomes
Published in Medicinal research reviews (01-01-2019)“…Serine/threonine kinases (STKs) represent the majority of discovered kinases to date even though a few Food and Drug Administration approved STKs inhibitors…”
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Diabetes mellitus: Classification, mediators, and complications; A gate to identify potential targets for the development of new effective treatments
Published in Biomedicine & pharmacotherapy (01-12-2023)“…Nowadays, diabetes mellitus has emerged as a significant global public health concern with a remarkable increase in its prevalence. This review article focuses…”
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P2Y1 Antagonists: Combining Receptor-Based Modeling and QSAR for a Quantitative Prediction of the Biological Activity Based on Consensus Scoring
Published in Journal of medicinal chemistry (12-07-2007)“…P2Y1 is an ADP-activated G protein-coupled receptor (GPCR). Its antagonists impede platelet aggregation in vivo and are potential antithrombotic agents…”
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Trifluoperazine, a Well-Known Antipsychotic, Inhibits Glioblastoma Invasion by Binding to Calmodulin and Disinhibiting Calcium Release Channel IP3R
Published in Molecular cancer therapeutics (01-01-2017)“…Calcium (Ca ) signaling is an important signaling process, implicated in cancer cell proliferation and motility of the deadly glioblastomas that aggressively…”
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Design, Synthesis and Biological Evaluation of 1,3,5-Triazine Derivatives Targeting hA1 and hA3 Adenosine Receptor
Published in Molecules (Basel, Switzerland) (22-06-2022)“…Adenosine mediates various physiological activities in the body. Adenosine receptors (ARs) are widely expressed in tumors and the tumor microenvironment (TME),…”
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Discovery of N-benzylbenzamide-based allosteric inhibitors of Aurora kinase A
Published in Bioorganic & medicinal chemistry (15-03-2024)“…[Display omitted] •Novel AurkA allosteric inhibitors of N-benzylbenzamide backbone were designed and synthesized.•The most potent analogue 6h (AurkA…”
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Sulfonamide-based 4-anilinoquinoline derivatives as novel dual Aurora kinase (AURKA/B) inhibitors: Synthesis, biological evaluation and in silico insights
Published in Bioorganic & medicinal chemistry (01-07-2020)“…Three series of 4-anilinoquinoline derivatives bearing a sulfonamide moiety (5a-d, 9a-d and 11a-d) were designed and synthesized as potential novel dual Aurora…”
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Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2-a]pyrimidine hybrids as potential anticancer agents with apoptosis inducing activity
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2023)“…Topoisomerases II are ubiquitous enzymes with significant genotoxic effects in many critical DNA processes. Additionally, epidermal growth factor receptor…”
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Scaffold Repurposing of In-House Small Molecule Candidates Leads to Discovery of First-in-Class CDK-1/HER-2 Dual Inhibitors: In Vitro and In Silico Screening
Published in Molecules (Basel, Switzerland) (01-09-2021)“…Recently, multitargeted drugs are considered a potential approach in treating cancer. In this study, twelve in-house indole-based derivatives were preliminary…”
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Reprofiling of pyrimidine-based DAPK1/CSF1R dual inhibitors: identification of 2,5-diamino-4-pyrimidinol derivatives as novel potential anticancer lead compounds
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2020)“…Hybridization of reported weakly active antiproliferative hit 5-amino-4-pyrimidinol derivative with 2-anilino-4-phenoxypyrimidines suggests a series of…”
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EGFR inhibitors from cancer to inflammation: Discovery of 4-fluoro-N-(4-(3-(trifluoromethyl)phenoxy)pyrimidin-5-yl)benzamide as a novel anti-inflammatory EGFR inhibitor
Published in Bioorganic chemistry (01-05-2019)“…[Display omitted] •Compound 4d is an anti-inflammatory EGFR inhibitor.•Compound 4d inhibits LPS-induced NO, IL-1β, IL-6 and TNF-α production.•Compound 4d…”
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Discovery of N-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide: a novel, selective, and competitive indole-based lead inhibitor for human monoamine oxidase B
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2020)“…Herein, two new series of N-substituted indole-based analogues were rationally designed, synthesized via microwave heating technology, and evaluated as…”
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Synthesis and structure–activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzheimer’s disease
Published in Bioorganic & medicinal chemistry letters (15-12-2012)“…A series of thiazole derivatives were designed, and prepared to develop RAGE antagonist for the treatment of Alzheimer’s disease (AD). SAR studies were…”
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Novel potent blockers for TWIK-1/TREK-1 heterodimers as potential antidepressants
Published in Biomedicine & pharmacotherapy (01-09-2023)“…TREK-1 (TWIK-related potassium channel-1) is a subunit of the two-pore domain potassium (K2p) channel and is widely expressed in the brain. TREK-1 knockout…”
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Identification of Novel Aryl Carboxamide Derivatives as Death-Associated Protein Kinase 1 (DAPK1) Inhibitors with Anti-Proliferative Activities: Design, Synthesis, In Vitro, and In Silico Biological Studies
Published in Pharmaceuticals (Basel, Switzerland) (25-08-2022)“…Death-associated protein kinase 1 (DAPK1) is a serine/threonine protein kinase involved in diverse fundamental cellular processes such as apoptosis and…”
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Caffeine-Mediated Inhibition of Calcium Release Channel Inositol 1,4,5-Trisphosphate Receptor Subtype 3 Blocks Glioblastoma Invasion and Extends Survival
Published in Cancer research (Chicago, Ill.) (01-02-2010)“…Calcium signaling is important in many signaling processes in cancer cell proliferation and motility including in deadly glioblastomas of the brain that…”
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Melatonin Analogues Potently Inhibit MAO-B and Protect PC12 Cells against Oxidative Stress
Published in Antioxidants (12-10-2021)“…Monoamine oxidase B (MAO-B) metabolizes dopamine and plays an important role in oxidative stress by altering the redox state of neuronal and glial cells. MAO-B…”
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Design, Synthesis, In Vitro, and In Silico Studies of New N5-Substituted-pyrazolo[3,4-d]pyrimidinone Derivatives as Anticancer CDK2 Inhibitors
Published in Pharmaceuticals (Basel, Switzerland) (11-11-2023)“…CDK2 is a key player in cell cycle processes. It has a crucial role in the progression of various cancers. Hepatocellular carcinoma (HCC) and colorectal cancer…”
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