The discovery, synthesis and in vitro activity of a novel series of rhodanine based phosphodiesterase-4 (PDE4) inhibitors is described. Structure-activity relationship studies directed toward improving potency led to the development of submicromolar inhibitors 2n and 3i (IC(50)=0.89 & 0.74 microM). The replacement of rhodanine with structurally related heterocycles was also investigated and led to the synthesis of pseudothiohydantoin 7 (IC(50)=0.31 microM).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2008.01.117 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
New thiazole derivative as a potential anticancer and topoisomerase II inhibitor.
Sci Rep
January 2025
Chemistry Department, Faculty of Science, Damietta University, Damietta, New-Damietta, 34517, Egypt.
To shed light on the significance of thiazole derivatives in the advancement of cancer medication and to contribute to therapeutic innovation, we have designed the synthesis and antiproliferative activity investigation of 5-(1,3-dioxoisoindolin-2-yl)-7-(4-nitrophenyl)-2-thioxo-3,7-dihydro-2H-pyrano[2,3-d] thiazole-6-carbonitrile, the structure of thiazole derivative was confirmed by spectroscopic techniques UV, IR and NMR. The cytotoxic activity (in vitro) of the new hybrid synthesized compound on five human cancer cell lines; human liver hepatocellular carcinoma (HepG-2), colorectal carcinoma (HCT-116), breast adenocarcinoma (MCF-7), and epithelioid carcinoma (Hela), and a normal human lung fibroblast (WI-38) was studied using MTT assay. The compound exhibited a strong cytotoxicity effect against HepG-2 and MCF-7.
View Article and Find Full Text PDFRhodanine-Piperazine Hybrids as Potential VEGFR, EGFR, and HER2 Targeting Anti-Breast Cancer Agents.
Int J Mol Sci
November 2024
Chair and Department of Organic Chemistry, Medical University of Lublin, 4A Chodzki Street, 20-093 Lublin, Poland.
Article Synopsis
- Breast cancer is a major health issue for women globally, prompting research for new treatments that specifically target proteins involved in tumor growth.
- Researchers developed and tested new compounds called rhodanine-piperazine hybrids aimed at key tyrosine kinases like VEGFR, EGFR, and HER2, identifying three that showed notable anticancer activity.
- One compound, in particular, demonstrated strong effectiveness against certain breast cancer cell lines and had favorable binding interactions with the target proteins, suggesting it could be a promising candidate for future drug development.
Exploring the rhodanine universe: Design and synthesis of fluorescent rhodanine-based derivatives as anti-fibrillar and anti-oligomer agents against α-synuclein and 2N4R tau.
Bioorg Med Chem
December 2024
Department of Basic Medical Sciences, College of Veterinary Medicine, Purdue University, West Lafayette, IN 47907, United States. Electronic address:
Tau and α-synuclein (α-syn) are prone-to-aggregate proteins that can be responsible for pathological lesions found in the brains of Alzheimer's disease (AD), Lewy body dementia (LBD), and Parkinson's disease (PD) patients. The early-stage oligomers and protofibrils of tau are believed to be strongly linked to human cognitive impairment while the toxic α-syn oligomers are associated with behavioral motor deficits. Therefore, concurrent targeting of both proteinaceous aggregates and oligomers are very challenging.
View Article and Find Full Text PDFRational design and synthesis of novel N-benzylindole-based epalrestat analogs as selective aldose reductase inhibitors: An unexpected discovery of a new glucose-lowering agent (AK-4) acting as a mitochondrial uncoupler.
Eur J Med Chem
January 2025
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, 54124, Greece. Electronic address:
Diabetes mellitus is one of the most frequent metabolic diseases associated with hyperglycemia. Although antidiabetic drugs reduce hyperglycemia, diabetic patients suffer from abnormal fluctuations in blood glucose levels leading to the onset of long-term complications. Aldose reductase inhibitors are considered a promising strategy for regulating the occurrence of diabetic-specific comorbidities.
View Article and Find Full Text PDFHeterocyclic compounds represent a prominent class of molecules with diverse pharmacological activities. Among their therapeutic applications, they have gained significant attention as carbonic anhydrase (CA) inhibitors, owing to their potential in the treatment of various diseases such as epilepsy, cancer and glaucoma. CA is a widely distributed zinc metalloenzyme that facilitates the reversible interconversion of carbon dioxide and bicarbonate.
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!