This paper describes the synthesis and the spectroscopic characterisation of cis-dichloro[N-(4-(17alpha-ethynylestradiolyl)-benzyl)-ethylenediamine]platinum(II) and cis-diamino[2-(4-(17alpha-ethynylestradiolyl)-benzoylamino)-malonato]platinum(II). These complexes were synthesised in good yield according to multi-step procedures based on the classical and non-classical Sonogashira coupling reaction, respectively. These compounds retain an acceptable degree of relative binding affinity (RBA) for the alpha form of estrogen receptor. Combined treatment of breast cancer cell lines, namely hormone-sensitive MCF-7 and hormone-insensitive MDA-MB-231 cell lines, indicates that these compounds maintain agonistic activity so that the potential advantage in vehiculation of the cytotoxic moiety by means of the receptor system is counteracted by the proliferative effect of the estrogenic component of the entire molecule, especially at low concentrations.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1039/b507716h | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
The potential of antibody-drug conjugates for effective therapy in diffuse large B-cell lymphoma.
Expert Opin Biol Ther
January 2025
OU Stephenson Cancer Center, Oklahoma City.
Introduction: Antibody-drug conjugates (ADCs) are a rapidly evolving class of anti-cancer drugs with a significant impact on management of hematological malignancies including diffuse large B-cell lymphoma (DLBCL). ADCs combine a cytotoxic drug (a.k.
View Article and Find Full Text PDFGinsenoside Re suppresses high glucose-induced apoptosis of placental trophoblasts through endoplasmic reticulum stress-related CHOP/GADD153.
Hum Exp Toxicol
January 2025
Department of Gynecology and Obstetrics, Fuyong People's Hospital, Shenzhen, China.
Gestational diabetes mellitus (GDM) is a metabolic disorder that arises during pregnancy and heightens the risk of placental dysplasia. Ginsenoside Re (Re) may stabilize insulin and glucagon to regulate glucose levels, which may improve diabetes-associated diseases. This study aims to investigate the mechanism of Re in high glucose (HG)-induced apoptosis of trophoblasts through endoplasmic reticulum stress (ERS)-related protein CHOP/GADD153.
View Article and Find Full Text PDFSilencing of FZD7 Inhibits Endometriotic Cell Viability, Migration, and Angiogenesis by Promoting Ferroptosis.
Cell Biochem Biophys
January 2025
Department of Obstetrics and Gynecology, Lishui Municipal Central Hospital, Lishui, Zhejiang, 323000, China.
Background: Endometriosis (EMS) is a difficult gynecological disease to cure. Frizzled-7 (FZD7) has been shown to be associated with the development of EMS, but its specific mechanism remains unclarified. This study aims to explore the role of FZD7 in EMS.
View Article and Find Full Text PDFConstruction of a Cas9-targeted mutagenesis mini-library in the upland cotton genetic standard line (TM-1).
Plant Cell Rep
January 2025
National Key Laboratory of Cotton Bio-Breeding and Integrated Utilization, Institute of Cotton Research of Chinese Academy of Agricultural Sciences, Anyang, 455000, Henan, China.
Suppressing the progression of bladder cancer using cyclovirobuxine D based on network pharmacology and bioinformatics approaches.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Urology, Affiliated Xi'an Peoples Hospital (Xi'an Fourth Hospital) of Northwest University, Xi'an, 710000, China.
Limited treatment options are available for bladder cancer (BCa) resulting in extremely high mortality rates. Cyclovirobuxine D (CVB-D), a naturally alkaloid, reportedly exhibits notable antitumor activity against diverse tumor types. However, its impact on CVB-D on BCa and its precise molecular targets remain unexplored.
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!