Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
According to the binding mode of ABBV-744 with bromodomains and the cape space of HDAC, the novel selective HDAC/BRD4 dual inhibitors were designed and synthesized by the pharmacophore fusion strategy. Evaluating the biomolecular activities through SARs exploration identified three kinds of selective dual inhibitors 41c (HDAC1/BRD4), 43a (pan-HDAC/BRD4) and 43d (HDAC6/BRD4(BD2)), whose target-related cellular activities in MV-4-11 cells were also confirmed. Significantly, the selective dual inhibitor 41c (HDAC1/BRD4) exhibited synergistic effects against MV-4-11 cells, which strongly induced G0/G1 cell cycle arrest and apoptosis, and the first HDAC6/BRD4(BD2) dual inhibitor was found. This study provides support for selective HDAC/BRD4 dual inhibitors as epigenetic probes based on pyrrolopyridone core for the future biological evaluation in different cancer cell lines.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2020.112868 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Ginsenoside Rh2 repressed the progression of prostate cancer through the mitochondrial damage induced by mitophagy and ferroptosis.
Front Oncol
August 2025
Department of Urology, Tianjin Institute of Urology, The Second Hospital of Tianjin Medical University, Tianjin, China.
Introduction: Prostate cancer (PC), the most common male genitourinary malignancy and second leading cause of global cancer deaths in men, frequently progresses to lethal castration-resistant PC (CRPC). Ginsenoside Rh2 (GRh2), a ginseng-derived bioactive compound, exhibits antitumor potential, but its efficacy and mechanisms in PC remain unclear.
Methods: PC3 cells were treated with GRh2 to assess proliferation (IC50 calculation), migration, and invasion.
Epigenetic regulation of bladder cancer in the context of aging.
Front Pharmacol
August 2025
Stem Cell Research Center, Department of Pathology and Pathophysiology, School of Medicine, Tongji University, Shanghai, China.
Bladder cancer (BC) is a disease that predominantly affects older adults, with aging playing a critical role in its onset and progression. Age-associated phenomena, including immunosenescence and chronic inflammation, form a pro-tumor milieu, while genomic instability and epigenetic drift further increase cancer risk. The review highlights the dual role of DNA methylation in BC: global hypomethylation can activate transposable elements and oncogenes, whereas focal hypermethylation silences tumor-suppressor genes like CDKN2A, especially detrimental in older tissues that rely on these genes for senescence control.
View Article and Find Full Text PDFAdvances in Tumor Microenvironment and Immunotherapeutic Strategies for Hepatocellular Carcinoma.
Oncol Res
September 2025
Department of Biliary-Pancreatic Surgery, Sun Yat-Sen Memorial Hospital, Sun Yat-Sen University, Guangzhou, 510120, China.
Hepatocellular carcinoma (HCC) is a highly aggressive malignancy, largely driven by an immunosuppressive tumor microenvironment (TME) that facilitates tumor growth, immune escape, and resistance to therapy. Although immunotherapy-particularly immune checkpoint inhibitors (ICIs)-has transformed the therapeutic landscape by restoring T cell-mediated anti-tumor responses, their clinical benefit as monotherapy remains suboptimal. This limitation is primarily attributed to immunosuppressive components within the TME, including tumor-associated macrophages, regulatory T cells (Tregs), and myeloid-derived suppressor cells (MDSCs).
View Article and Find Full Text PDFSynthesis and Computational Evaluation of ‑Acetyl-Derived Schiff Bases Incorporating 1,2,4-Triazoles for Dual Inhibition of Prostate Cancer Cells and Carbonic Anhydrases.
ACS Omega
September 2025
Department of Chemistry, Faculty of Arts and Sciences, Kafkas University, 36040 Kars, Turkey.
In this study, we synthesized a series of novel -acetyl Schiff bases (-) containing 1,2,4-triazole moiety and evaluated their potential as anticancer agents through both experimental and computational approaches. Cytotoxicity assays on prostate cancer (PC) (DU145) and normal epithelial cells (PNT1a) demonstrated selective inhibition, particularly for compounds , , and , with IC values of 73.25, 49.
View Article and Find Full Text PDFDesign, Synthesis, and Molecular Docking Studies of Novel Pyrazoline-Thiazoles as Cholinesterase Dual-Target Inhibitors for the Treatment of Alzheimer's Disease.
ACS Omega
September 2025
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey.
Ten novel pyrazoline-thiazole derivatives were synthesized and assessed for their potential as acetylcholinesterase and butyrylcholinesterase inhibitors. The structure of the target compounds was characterized by H NMR and C NMR, and purity was determined using HPLC. The in vitro enzyme inhibitory activity assays determined that compounds (IC = 0.
View Article and Find Full Text PDF