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Antitumor properties of certain spirooxindoles towards hepatocellular carcinoma endowed with antioxidant activity.
- Source :
-
Journal of enzyme inhibition and medicinal chemistry [J Enzyme Inhib Med Chem] 2020 Dec; Vol. 35 (1), pp. 831-839. - Publication Year :
- 2020
-
Abstract
- In the current medical era, spirooxindole motif stands out as a privileged heterospirocyclic scaffold that represents the core for a wide range of bioactive naturally isolated products (such as Strychnofoline and spirotryprostatins A and B) and synthetic compounds. Interestingly, no much attention has been paid to develop spirooxindole derivatives with dual antioxidant and anticancer activities. In this context, a series of spirooxindoles 6a-p was examined for their anticancer effect towards HepG2 hepatocellular carcinoma and PC-3 prostate cancer cell lines. Spirooxindole 6a was found to be an efficient anti-proliferative agent towards both HepG2 and PC-3 cells (IC50 = 6.9 and 11.8 µM, respectively). Afterwards, spirooxindole 6a was assessed for its apoptosis induction potential in HepG2 cells, where its pro-apoptotic impact was approved via the significant elevation in the Bax/Bcl-2 ratio and the expression levels of caspase-3.
- Subjects :
- Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Antioxidants chemical synthesis
Antioxidants chemistry
Apoptosis drug effects
Biphenyl Compounds antagonists & inhibitors
Carcinoma, Hepatocellular metabolism
Carcinoma, Hepatocellular pathology
Cell Proliferation drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Hep G2 Cells
Humans
Liver Neoplasms metabolism
Liver Neoplasms pathology
Molecular Structure
Oxindoles chemical synthesis
Oxindoles chemistry
PC-3 Cells
Picrates antagonists & inhibitors
Spiro Compounds chemical synthesis
Spiro Compounds chemistry
Structure-Activity Relationship
Tumor Cells, Cultured
Antineoplastic Agents pharmacology
Antioxidants pharmacology
Carcinoma, Hepatocellular drug therapy
Liver Neoplasms drug therapy
Oxindoles pharmacology
Spiro Compounds pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1475-6374
- Volume :
- 35
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of enzyme inhibition and medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 32208781
- Full Text :
- https://doi.org/10.1080/14756366.2020.1743281