We report the synthesis and the pharmacological evaluation of a new class of human carbonic anhydrase (hCA) inhibitors prepared regio- and stereoselectively by reacting sulfanilamide with ethyl trans-phenylglycidate in the presence of cobalt(II) chloride. Various derivatizations of the ester moiety in the parent compound led to a small library of derivatives (2R,3R and 2S,3S) which displayed interesting inhibitory activities towards the human tumor-associated isoform CA IX. One of the new compounds shows high selectivity in inhibiting hCA IX compared to the two physiologically relevant, cytosolic isozymes hCA I and hCA II. A molecular modeling study was conducted in order to simulate the binding mode of this new family of enzyme inhibitors within the active sites of hCA IX and hCA II.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.ejmech.2008.03.034 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Catheter-directed therapy for pulmonary embolism in pediatrics: a systematic review and meta-analysis.
Thromb J
January 2025
Pediatric Emergency Department, St. Christopher's Hopsoital for Children, Philadelphia, PA, USA.
Background: Acute pulmonary embolism (PE) is a serious and potentially fatal condition that is relatively rare in the pediatric population. In patients presenting with massive/submassive PE, catheter-directed Therapy (CDT) presents an emerging therapeutic modality by which PE can be managed.
Methods: Electronic databases were systematically searched through May 2024.
Prenatal inflammation impairs early CD11c-positive microglia induction and delays myelination in neurodevelopmental disorders.
Commun Biol
January 2025
Department of Obstetrics and Gynecology, Nagoya University Graduate School of Medicine, Nagoya, Japan.
Histological chorioamnionitis (HCA) is a form of maternal immune activation (MIA) linked to an increased risk of neurodevelopmental disorders in offspring. Our previous study identified neurodevelopmental impairments in an MIA mouse model mimicking HCA. Thus, this study investigated the role of CD11c microglia, key contributors to myelination through IGF-1 production, in this pathology.
View Article and Find Full Text PDFSulphonyl thiourea compounds containing pyrimidine as dual inhibitors of I, II, IX, and XII carbonic anhydrases and cancer cell lines: synthesis, characterization and studies.
RSC Med Chem
December 2024
VNU University of Education, Vietnam National University, Hanoi 144 Xuan Thuy, Cau Giay Ha Noi Vietnam.
Some novel sulphonyl thiourea derivatives (7a-m) containing 4,6-diarylpyrimidine rings were designed and synthesized using a one-pot procedure. These compounds exhibited remarkable dual inhibitory activity against human carbonic anhydrase CA I, CA II, CA IX, and XII isoenzymes and some cancer cell lines. Among them, some thioureas had significantly more potent inhibitory activities in the order of 7l > 7c > 7f (against the CA I isoform), 7f > 7b > 7c (against the CA II isoform), 7c > 7g > 7a > 7b (against the CA IX isoform), and 7d > 7c > 7g > 7f (against the CA XII isoform).
View Article and Find Full Text PDFRepeat breast-conserving surgery (BCS) for in breast tumor recurrence after initial BCS for ductal carcinoma .
Gland Surg
December 2024
The London Breast Institute, Princess Grace Hospital, London, UK.
Factors Associated with the Use of Complementary and Alternative Medicine in Rural Northern Victoria, Australia.
Health Care Anal
January 2025
Macarthur Clinical School, Western Sydney University, Locked Bag, Penrith, NSW, 1797, Australia.
About one-third of Australians use the services of complementary and alternative medicine (CAM); but debate about the role of CAM in public healthcare is vociferous. Despite this, the mechanisms driving CAM healthcare choices are not well understood, especially in rural Australia. From 2016 to 2018, 2,679 persons from the Goulburn Valley, northern Victoria, were surveyed, 28% (755) of whom reporting visiting CAM practitioners.
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!