Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2006.03.098 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Explanatory review on DDR inhibitors: their biological activity, synthetic route, and structure-activity relationship.
Mol Divers
January 2025
Integrated Drug Discovery Centre, Department of Pharmaceutical Chemistry, Acharya & BM Reddy College of Pharmacy, Bengaluru, 560107, Karnataka, India.
Discoidin domain receptors (DDR) are categorized under tyrosine kinase receptors (RTKs) and play a crucial role in various etiological conditions such as cancer, fibrosis, atherosclerosis, osteoarthritis, and inflammatory diseases. The structural domain rearrangement of DDR1 and DDR2 involved six domains of interest namely N-terminal DS, DS-like, intracellular juxtamembrane, transmembrane juxtamembrane, extracellular juxtamembrane intracellular kinase domain, and the tail portion contains small C-tail linkage. DDR has not been explored to a wide extent to be declared as a prime target for any particular pathological condition.
View Article and Find Full Text PDFDiscovery of DCAF16 Binders for Targeted Protein Degradation.
ACS Chem Biol
January 2025
Department of Chemistry, Northwestern University, Evanston, Illinois 60208, United States.
Conventional small-molecule drugs primarily operate by inhibiting protein function, but this approach is limited when proteins lack well-defined ligand-binding pockets. Targeted protein degradation (TPD) offers an alternative approach by harnessing cellular degradation pathways to eliminate specific proteins. Recent studies have expanded the potential of TPD by identifying additional E3 ligases, with DCAF16 emerging as a promising candidate for facilitating protein degradation through both proteolysis-targeting chimera (PROTAC) and molecular glue mechanisms.
View Article and Find Full Text PDFCD44-Receptors-Mediated Multiprong Targeting Strategy Against Breast Cancer and Tumor-Associated Macrophages: Design, Optimization, Characterization, and Cytologic Evaluation.
Int J Nanomedicine
January 2025
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, 11451 Saudi Arabia.
Introduction: Owing to its high prevalence, colossal potential of chemoresistance, metastasis, and relapse, breast cancer (BC) is the second leading cause of cancer-related fatalities in women. Several treatments (eg, chemotherapy, surgery, radiations, hormonal therapy, etc.) are conventionally prescribed for the treatment of BC; however, these are associated with serious systemic aftermaths.
View Article and Find Full Text PDFAugmented silver sulfadiazine nanostructured lipid carriers impregnated collagen sponge for promoting burn wound healing.
Int J Biol Macromol
January 2025
Department of Pharmaceutics, Faculty of Pharmacy, University of Sadat City, P.O. Box 32897, Menoufia, Egypt; Nanomedicine Laboratory, Faculty of Pharmacy, University of Sadat City, P.O. Box 32897, Sadat City, Egypt. Electronic address:
Silver sulfadiazine (SSD) is a widely used antibacterial agent for burn wound treatment owing to its capability in re-epithelialization and wound healing. However, due to its low solubility, the need for an effective drug delivery system is mandatory. This study aimed to optimize SSD nanostructured lipid-based carriers (NLCs), incorporated in a collagen sponge form as an innovative topical dosage form for effective burn wound treatment.
View Article and Find Full Text PDFElectrochemically Driven Selective Olefin Epoxidation by Cobalt-TAML Catalyst.
J Am Chem Soc
January 2025
Department of Chemistry, Korea University, 145 Anam-ro, Seongbuk-gu, Seoul 02841, South Korea.
Epoxides are versatile chemical intermediates that are used in the manufacture of diversified industrial products. For decades, thermochemical conversion has long been employed as the primary synthetic route. However, it has several drawbacks, such as harsh and explosive operating conditions, as well as a significant greenhouse gas emissions problem.
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!