Natural pterocarpans and synthetic 5-carba-pterocarpans are isosteres in which the oxygen atom at position 5 in the pyran-ring of pterocarpans is replaced by a methylene group. These 5-carba-analogues were obtained in good yields through the palladium-catalyzed oxyarylation of alcoxy-1,2-dihydronaphthalens with o-iodophenols in PEG-400. They were evaluated on human cancer cell lineages derived respectively from prostate tumor (PC3, IC = 11.84 μmol L, SI > 12)) and acute myeloid leukemia (HL-60, IC = 8.81 μmol L, SI > 16), highly incident cancer types presenting resistance against traditional chemotherapeutics. Compound 6c (LQB-492) was the most potent (IC = 3.85 μmol L, SI > 37) in SF-295 cell lineage (glioblastoma). Such findings suggest that 5-carba-pterocarpan can potentially be new hit compounds for further development of novel antiproliferative agents.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bioorg.2020.104584 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Comparative Analysis of 4NQO- and Ethanol-Induced Oral Epithelial Dysplasia and Oral Squamous Cell Carcinoma in Male and Female Mice: Association With Peripheral Blood Inflammatory Markers.
J Oral Pathol Med
January 2025
Department of Oral and Maxillofacial Pathology, Federal University of Uberlândia, Uberlândia, Minas Gerais, Brazil.
Background: Considering that peripheral blood biomarkers are prognostic predictors for several human tumors, this study aimed to comparatively analyze the association of hematological alterations with the incidence of epithelial dysplasia (ED) and oral squamous cell carcinoma (OSCC) in male and female mice treated with 4-nitroquinoline-N-oxide (4NQO) and ethanol (EtOH).
Methods: 120 C57Bl/6J mice (60 males and 60 females) were allocated to four groups (n = 15). They were treated firstly either with 5 mg/mL propylene glycol (PPG) or 100 μg/mL 4NQO in the drinking water for 10 weeks, followed by sterilized water (HO) or 8% EtOH (v/v) for 15 weeks, as follows: PPG/HO, PPG/EtOH, 4NQO/HO, and 4NQO/EtOH (CEUA-UFU, #020/21).
Targeting p38γ synergistically enhances sorafenib-induced cytotoxicity in hepatocellular carcinoma.
Cell Biol Toxicol
January 2025
Division of Abdominal Tumor Multimodality Treatment, Cancer Center and Laboratory of Molecular Targeted Therapy in Oncology, West China Hospital, Sichuan University, 610041, Chengdu, Sichuan Province, China.
Sorafenib (Sora) is a first-line treatment for patients with advanced hepatocellular carcinoma (HCC). It can significantly improve the survival rate of patients with advanced HCC, but it is prone to drug resistance during treatment, so the therapeutic effect is extremely limited. Here, we demonstrate that an elevated expression of protein kinase p38γ in hepatocellular carcinoma cells diminishes the tumor cells' sensitivity to Sora.
View Article and Find Full Text PDFEffect of terahertz radiation on cells and cellular structures.
Front Optoelectron
January 2025
Institute of Physics, Saratov State University, Saratov, 410012, Russia.
The paper presents the results of modern research on the effects of electromagnetic terahertz radiation in the frequency range 0.5-100 THz at different levels of power density and exposure time on the viability of normal and cancer cells. As an accompanying tool for monitoring the effect of radiation on biological cells and tissues, spectroscopic research methods in the terahertz frequency range are described, and attention is focused on the possibility of using the spectra of interstitial water as a marker of pathological processes.
View Article and Find Full Text PDFThe citizen perspective on challenges and rehabilitation needs among individuals treated for head and neck cancer: a qualitative study.
Support Care Cancer
January 2025
Clinical Nursing Research Unit, Aalborg University Hospital & Department of Clinical Medicine, Aalborg University, Aalborg, Denmark.
Purpose: In Denmark, the prevalence of head and neck cancer is approximately 17.000, and the incidence is increasing. The disease and treatment of this condition may lead to severe physical, psychological, and social consequences.
View Article and Find Full Text PDFExploring the role of multimodal [F]F-PSMA-1007 PET/CT and multiparametric MRI data in predicting ISUP grading of primary prostate cancer.
Eur J Nucl Med Mol Imaging
January 2025
The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, 325000, China.
Purpose: The study explores the role of multimodal imaging techniques, such as [F]F-PSMA-1007 PET/CT and multiparametric MRI (mpMRI), in predicting the ISUP (International Society of Urological Pathology) grading of prostate cancer. The goal is to enhance diagnostic accuracy and improve clinical decision-making by integrating these advanced imaging modalities with clinical variables. In particular, the study investigates the application of few-shot learning to address the challenge of limited data in prostate cancer imaging, which is often a common issue in medical research.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!