The first total synthesis of a unique flavone natural product, desmosdumotin B (1), was accomplished. Furthermore, three novel flavonoids, 6-8, and a novel chalcone, 9, were synthesized. The new compounds were evaluated as in vitro inhibitors of human cancer cell growth. The synthetic 1 showed significant cytotoxic activity against a multi-drug resistant cell line (KB-VIN) with an ED50 value of 2.0 microg/mL compared to >40 microg/mL against the parental KB cell line. Flavone 7 displayed selective activity against 1A9 ovarian carcinoma with an ED50 value of 0.7 microg/mL. Selected 1-analogs and synthetic intermediates were also screened for antitumor-promoting effects as inhibitors of EBV-EA activation. Among them, trihydroxyacetophenone derivatives 11 and 14 showed good activity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2005.04.070 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Aerobic exercise attenuates high-fat diet-induced glycometabolism impairments in skeletal muscle of rat: role of EGR-1/PTP1B signaling pathway.
Nutr Metab (Lond)
December 2024
College of Physical Education and Health Sciences, Zhejiang Normal University, 688 Yingbin Road, Jinhua, 321004, Zhejiang Province, China.
Objective: Impaired skeletal muscle glycogen synthesis contributes to insulin resistance (IR). Aerobic exercise reported to ameliorate IR by augmenting insulin signaling, however the detailed mechanism behind this improvement remains unclear. This study investigated whether aerobic exercise enhances glycogen anabolism and insulin sensitivity via EGR-1/PTP1B signaling pathway in skeletal muscle of rats.
View Article and Find Full Text PDFZinc finger proteins facilitate adaptation of a global insect pest to climate change.
BMC Biol
December 2024
State Key Laboratory for Ecological Pest Control of Fujian and Taiwan Crops, Institute of Applied Ecology, Fujian Agriculture and Forestry University, Fuzhou, 350002, China.
Background: Global climate change significantly impacts ecosystems, particularly through temperature fluctuations that affect insect physiology and behavior. As poikilotherms, insect pests such as the globally devastating diamondback moth (DBM), Plutella xylostella, are especially vulnerable to rising temperatures and extreme heat events, necessitating effective adaptive mechanisms.
Results: Here we demonstrate the roles of zinc finger proteins (ZFPs) in mediating thermal adaptability in DBM.
Effect of Oral Nutritional Supplements Composed of High Protein on Body Weight Loss After Gastrectomy.
In Vivo
December 2024
Department of Gastroenterological Surgery, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama, Japan.
Background/aim: Body weight loss (BWL) after gastrectomy for gastric cancer (GC) decreases postoperative quality of life and survival in patients with GC. This study aimed to evaluate the effect of oral nutritional supplements composed of high protein on BWL in the early period following gastrectomy.
Patients And Methods: Pre- and postoperative body weight and skeletal muscle mass were measured using bioelectrical impedance analysis in patients undergoing radical gastrectomy for GC and analyzed retrospectively.
Gene Expression Profiles in Ovarian Cancer Tissues as a Potential Tool to Predict Platinum-based Chemotherapy Resistance.
Anticancer Res
January 2025
Department of Pathology, Herlev Hospital, University of Copenhagen, Herlev, Denmark
Background/aim: Ovarian cancer (OC) is one of the leading gynecological causes of death among women. The current standard treatment for OC is debulking surgery followed by platinum-based chemotherapy treatments; however, despite initial success to treatment many patients experience relapses. Currently, there are no available tests to predict sensitivity or resistance to chemotherapy.
View Article and Find Full Text PDFRelationship Between F-FDG-PET/CT-derived Tumor Glucose Metabolic Activity, Nutritional Risk, and Survival in Patients With Soft-tissue Sarcoma.
Anticancer Res
January 2025
Department of Orthopedic Surgery, Graduate School of Medicine, University of the Ryukyus, Okinawa, Japan.
Background/aim: The present study aimed to assess the relationship between the maximum standardized uptake value (SUVmax) on F-fluorodeoxyglucose positron emission tomography computed tomography (F-FDG-PET/CT) and the geriatric nutritional risk index (GNRI) in patients with soft-tissue sarcomas (STSs).
Patients And Methods: The present single-center retrospective observational study included patients who underwent F-FDG-PET/CT and for whom serum albumin levels, height, and body weight were measured prior to therapeutic intervention.
Results: A total of 81 patients were included in the study.
Want 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!