A series of novel 1,3,4-thiadiazole-containing benzisoselenazolone derivatives were prepared by the condensation of 2-chloroselenobenzoyl chloride and 2-amino-5-substituted-1,3,4-thiadiazole. Their in vitro antiproliferative activities were evaluated in SSMC-7721, MCF-7 and A-549 cells. The results suggest that, in different tumor cells, some compounds have good antiproliferative activity, certain selectivity and potential value of further research.
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http://dx.doi.org/10.1016/j.bmcl.2012.03.043 | DOI Listing |
Int J Mol Sci
January 2023
Department of Bioorganic Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.
Ebselen is a low-molecular-weight organoselenium compound that has been broadly studied for its antioxidant, anti-inflammatory, and cytoprotective properties. These advantageous properties were initially associated with mimicking the activity of selenoprotein glutathione peroxidase, but the biomedical impact of this compound appear to be far more complex. Ebselen serves as a substrate or inhibitor with multiple protein/enzyme targets, whereas inhibition typically originates from the covalent modification of cysteine residues by opening the benzisoselenazolone ring and S-Se bond formation.
View Article and Find Full Text PDFJ Exp Clin Cancer Res
August 2021
Digestive Diseases Center, The Seventh Affiliated Hospital, Sun Yat-sen University, 518107, Shenzhen, Guangdong, China.
Background: Oxaliplatin is one of the most commonly used chemotherapeutic agent for the treatment of various cancers, including gastric cancer. It has, however, a narrow therapeutic index due to its toxicity and the occurrence of drug resistance. Hence, it is of great significance to develop novel therapies to potentiate the anti-tumor effect and reduce the toxicity of oxaliplatin.
View Article and Find Full Text PDFJ Biomol Struct Dyn
November 2022
Department of Microbiology, School of Sciences (SOS), Federal University of Technology Akure, Akure, Nigeria.
The dysregulation of cyclin-CDK6 interactions has been implicated in human breast cancer, providing a rationale for more therapeutic options. Recently, ATP-competitive inhibitors have been employed for managing breast cancer. These molecules, like most natural CDKs inhibitors, potently bind in the ATP-binding site of CDK6 to regulate trans-activation.
View Article and Find Full Text PDFSteroids
December 2019
Guangxi Key Laboratory of Natural Polymer Chemistry and Physics, Nanning Normal University, Nanning 530001, PR China. Electronic address:
The two different types of steroidal benzisoselenazolone hybrids were synthesized by incorporating benzisoselenazolone scaffold into dehydroepiandrosterone and B-norcholesterol. The antiproliferative activity of the synthesized compounds against some carcinoma cell lines were investigated. The results showed that some of these compounds have better inhibitory activity than abiraterone on the proliferation of tumor cells associated with human growth hormone, and have less cytotoxicity on normal human cells.
View Article and Find Full Text PDFMolecules
August 2019
Division of Organic Chemistry, Centre of Molecular and Macromolecular Studies, Polish Academy of Science, Sienkiewicza, 112, 90-363 Lodz, Poland.
A series of variously functionalized selenium-containing compounds were purposely synthesized and evaluated against a panel of cancer cell lines. Most of the compounds showed an interesting cytotoxicity profile with compound showing a potent activity on MCF7 cells. The ethyl amino derivative acts synergistically with -platin and inhibits the GST enzyme with a potency that well correlates with the cytotoxicity observed in MCF7 cells.
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