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European Journal of Medicinal Chemistry Reports
Scopus
ISSN 2772-4174 · Elsevier · 341 artikel di indeks
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Artikel Jurnal
Fragment-based discovery of novel small molecule targeting human BAG3
Bcl-2-associated athanogene 3 (BAG3) is a multifunctional co-chaperone protein that regulates apoptosis, autophagy, and proteostasis through interactions with HSP70 and other partners. Overexpression of BAG3 contributes to tumor cell survival, metastasis, and chemotherapy resistance, making it an…
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Artikel Jurnal
Endoperoxides in combating bacterial infections: synthetic pathways, mechanism, biological activity and mode of action
Endoperoxides are heterocyclic compounds with a peroxide functional group embedded in one or more rings. These compounds have gathered significant interest in the last two decades owing to their biological activities and pharmaceutical relevance. The most prominent endo-peroxide with…
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Artikel Jurnal
Design, synthesis and antiproliferative activity evaluation of new 3,7-disubstituted pyrrolo[2,3-c]pyridines
A number of 3,7-disubstituted 6-azaindoles were designed and synthesized starting from the readily accessible 2-chloro-3-nitro-4-picoline. The target compounds were tested for their antiproliferative activity against HT-1080, A431 and A549 cancer cell lines in comparison to the normal human AG01523…
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Artikel Jurnal
Naringin exhibits adaptogen-like and neuroprotective effects on mice under chronic stress, reversing cortical neuroinflammation and neurodegeneration
Chronic unpredictable mild stress (CUMS) induces impairment in cortical functional connectivity, which plays an important role in depression and anxiety. It remains unclear if naringin, a natural adaptogen with antidepressant and anxiolytic effects, reverses CUMS-induced depression by normalizing…
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Artikel Jurnal
Chemistry and pharmacology of naamine and naamidine-type marine alkaloids: an update
The marine alkaloids naamine A and naamidine A were first isolated from a calcareous sponge forty years ago. Since 1987, about 40 related natural products have been discovered in this series, including naamines A-G, isonaamines A-D, naamidines A-K, isonaamidines A-E, pyronaamidine, spironaamidine…
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Artikel Jurnal
Imidazole‒sulfonamide hybrid conjugate: A privilege scaffold with significant therapeutic potential
Combining two or more biologically active moieties in a single structure recently became one of the most proposed concepts that have been adopted in drug development process. Enhanced efficacy, limited side effects and declined drug resistance are the main features of molecular hybridization…
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Artikel Jurnal
Exploiting the synergy between computational and experimental biophysics for efficient cancer drug development
Targeted cancer therapies have revolutionized oncology by developing treatments that specifically target cancer cells, reducing side effects. However, traditional drug discovery approaches are often hindered by high costs, long timelines, and low success rates. To address these challenges, the…
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Artikel Jurnal
Inhibition of ginsenoside Re on pulmonary fibrosis induced by bleomycin in mice: Involved in modulating the CX3CL1/CX3CR1 axis
Pulmonary fibrosis (PF) is a common pathological feature of a variety of diffuse, progressive and irreversible pulmonary interstitial diseases, and effective therapeutic agents are currently lacking. Our previous study found that the total ginsenosides can improve pulmonary fibrosis induced by…
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Artikel Jurnal
Mechanisms of Panax notoginseng in the treatment of vascular disease: A review and preliminary analysis
Panax notoginseng, an essential Traditional Chinese Medicine (TCM), has been used to treat various vascular diseases, which are becoming widely recognized. However, there is a dearth of summary information regarding the therapeutic mechanism of notoginseng in the treatment of vascular diseases…
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Artikel Jurnal
Synthetic developments and biological insights of 1,2,3-triazoles: Unravelling scope for drug discovery
1,2,3-Triazoles have emerged as instrumental heterocyclic scaffolds playing key role in the field of synthetic and medicinal chemistry. The recent advancements utilizing the evolving technologies and the subsequent development of various synthetic strategies have dragged the attention based on…
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Artikel Jurnal
Sanguinarine alleviates cisplatin-induced apoptosis in AKI by upregulating BCL-2 through targeting the gene promoter i-motif
Acute kidney injury (AKI) is a severe clinical condition with high morbidity and mortality. Apoptosis of renal tubular epithelial cells is a key pathological driver, and upregulation of the anti-apoptotic protein BCL-2 is a validated protective mechanism. The BCL-2 promoter harbors a C-rich…
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Artikel Jurnal
Elucidating the mechanism of anti-ischemic stroke action of Irisflorentin:A combined approach using network pharmacology, molecular docking, and in vitro validation
Irisflorentin, an isoflavonoid isolated from Belamcanda chinensis (L.) Redouté, serves as a key bioactive molecule in Sagittaria, exhibiting antioxidative, hypoglycemic, and anti-inflammatory properties. Despite these attributes, the precise roles and mechanisms of Irisflorentin in mitigating…
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Artikel Jurnal
N-Acylhydrazones: applications and advances in drug discovery
N-Acylhydrazones (NAHs) represent a structurally versatile and pharmacologically active class of compounds widely explored over last two decades in medicinal chemistry. Characterized by the presence of both hydrazide and imine functionalities, NAHs exhibit a rich spectrum of biological activities…
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Artikel Jurnal
Nitrofuranyl derivatives as promising antitubercular agents: Structural insights and drug discovery perspectives
The emergence of MDR (multidrug-resistant) and XDR (extensively drug-resistant) variants of Mycobacterium tuberculosis has contributed to the universal resurgence of tuberculosis (TB). Nitrofuran-based compounds, traditionally used as antibacterial agents, have recently gained attention for their…
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Artikel Jurnal
Evaluation of the hepatoprotective properties of Vitex Altissima bark extracts and isolated bioactive: In-vitro and In-vivo approach
Vitex altissima (V. altissima), an ethnopharmacologically valuable plant, is explicitly used as traditional medicine by local folks to cure liver-related disorders in Coorg. Hence, the present study aimed to evaluate the bark extract's hepatoprotective and antioxidant mechanisms and its isolated…
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Artikel Jurnal
Peptide-mediated modulation of miRNAs: A novel therapeutic strategy for cancer
MicroRNAs are essential post-transcriptional regulators of gene expression, playing dual roles in oncogenesis as either oncogenes or tumour suppressors. Aberrant miRNA expression is a critical factor in cancer progression, influencing tumour development, metastasis, resistance to apoptosis, and…
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Artikel Jurnal
Synthesis, structure, photophysical, photochemical, and biological properties of hybrid macrocyclic structures containing two naphthalene moieties and a tri(ethylene glycol) tether
The structure of some promising crown ether-paracyclophane hybrid macrocyclic derivatives showing remarkable cytotoxicity was modified by replacing the two phenyl rings with naphthalene units. The synthesis of the newly designed macrocyclic derivatives was accomplished by applying the previously…
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Artikel Jurnal
Cinnamyl-driven GPR183 antagonists: Scaffold optimization toward non-opioid pain therapy
GPR183, a G protein-coupled receptor, has been implicated in the development and progression of neuropathic pain. Herein, we report the identification and characterization of a GPR183 antagonist, SLU-0012011. This compound inhibited GPR183 activation in a calcium mobilization assay and reduced…
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Artikel Jurnal
Preclinical validation of AMPDA-HB derivatives integrating Hsp70-specific TPP motif and anti-CD2 single domain antibody radiolabeled by Al
Background: Al(III) complexes are gaining increasing interest for their potential use in Positron Emission Tomography (PET) imaging by formation of ternary complexes with the radioisotope fluorine-18 ( 18 F). The non-macrocyclic semi-rigid pentadentate chelator AMPDA-HB has been recently proposed…