Steroids are classes of natural products widely distributed in nature, which have been demonstrated to exhibit broad biological functions, and have also attracted increasing interest from bioorganic and pharmaceutical researches. In order to develop novel chemical entities as potential cytotoxic agents, a series of steroidal isatin conjugations derived from epiandrosterone and androsterone were efficiently prepared and characterized, and all these obtained compounds were screened for their potential cytotoxic activities. The preliminary bioassay indicated that most of the newly synthesized compounds exhibited good cytotoxic activities against human gastric cancer (SGC-7901), melanoma (A875), and hepatocellular liver carcinoma (HepG2) cell lines compared with 5-fluorouracil (5-FU), which might be considered as promising scaffold for further development of potential anticancer agents.
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http://dx.doi.org/10.1080/14756366.2019.1659790 | DOI Listing |
Future Med Chem
January 2025
Department of Chemistry and Biochemistry, Augusta University, Augusta, GA, USA.
Aims: This study aimed to develop novel molecular hybrid conjugates integrating isatin, rhodanine, and phthalimide pharmacophores to create effective analgesic and anti-inflammatory agents with improved safety profiles over existing treatments.
Materials & Methods: A series of hybrid conjugates () were synthesized and evaluated through in vitro and in vivo biological assays. The most promising compound, , underwent extensive pharmacological and toxicological evaluations.
Molecules
November 2023
Faculty of Chemistry, Inorganic Chemistry, Technical University Dortmund, Otto-Hahn-Strasse 6, 44227 Dortmund, Germany.
In a sustained search for novel potential drug candidates with multispectrum therapeutic application, a series of novel spirooxindoles was designed and synthesized via regioselective three-component reaction between isatin derivatives, 2-phenylglycine and diverse arylidene-imidazolidine-2,4-diones (Hydantoins). The suggested stereochemistry was ascertained by an X-ray diffraction study and NMR spectroscopy. The resulting tetracyclic heterocycles were screened for their in vitro in vivo anti-inflammatory and analgesic activity and for their in vitro antimicrobial potency.
View Article and Find Full Text PDFJ Steroid Biochem Mol Biol
July 2022
Faculty of Pharmacy, Osaka-Ohtani University, Osaka 584-8540, Japan.
Most members of the aldo-keto reductase (AKR) 1 C subfamily are hydroxysteroid dehydrogenases (HSDs). Similarly to humans, four genes for AKR1C proteins (AKR1C1-AKR1C4) have been identified in the pig, which is a suitable species for biomedical research model of human diseases and optimal organ donor for xenotransplantation. Previous study suggested that, among the porcine AKR1Cs, AKR1C1 and AKR1C4 play important roles in steroid hormone metabolism in the reproductive tissues; however, their biological functions are still unknown.
View Article and Find Full Text PDFAdv Exp Med Biol
January 2022
Department of Pharmacy, Birla Institute of Technology & Science, Pilani, Vidyavihar, Rajasthan, India.
Ten novel isatin Schiff base analogs have been designed using a combination of isatin, hydrazine hydrate, and para-dimethylaminobenzaldehyde. Molecular docking studies have been performed to study the binding interactions of the designed compounds with COX-2 protein as a target (PDB code: 3LN1). The ten novel 3-({p-dimethylamino}benzylidenehydrazinylidene)-1,3-dihydro-2H-indole-2-one derivatives (IIIa-IIIj) were synthesized.
View Article and Find Full Text PDFInt J Cancer
February 2021
Section of Nutrition and Metabolism, International Agency for Research on Cancer (IARC-WHO), Lyon, France.
Hepatocellular carcinoma (HCC) development entails changes in liver metabolism. Current knowledge on metabolic perturbations in HCC is derived mostly from case-control designs, with sparse information from prospective cohorts. Our objective was to apply comprehensive metabolite profiling to detect metabolites whose serum concentrations are associated with HCC development, using biological samples from within the prospective European Prospective Investigation into Cancer and Nutrition (EPIC) cohort (>520 000 participants), where we identified 129 HCC cases matched 1:1 to controls.
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