(1-2-bis(1-2-benzisoselenazolone-3(2h)-ketone))ethane has been researched along with Neoplasms* in 2 studies
2 other study(ies) available for (1-2-bis(1-2-benzisoselenazolone-3(2h)-ketone))ethane and Neoplasms
| Article | Year |
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Synthesis and in vitro antiproliferative evaluation of novel hybrids from 1,3,4-thiadiazole and benzisoselenazolone.
Novel hybrids from 1,3,4-thiadiazole and benzisoselenazolone were designed, synthesized and evaluated for their in vitro antiproliferative activities by CCK-8 assay against three types of human cancer cell lines, SMMC-7721, MCF-7 and A549 cells. The preliminary bioassay results demonstrated that all tested compounds 4a-p showed potent antiproliferative activities, and some compounds exhibited better effects than positive control ethaselen and 5-fluorouracil (5-FU) against various cancer cell lines. Furthermore, compound 4g showed significant antiproliferative activities against SMMC-7721 cells with an IC50 value of 2.08 µM. Compounds 4b and 4m displayed highly effective biological activities against MCF-7 cells with an IC50 values of 2.03 and 2.06 µM, respectively. Compound 4i exhibited the best inhibitory effect against A549 cells with an IC50 value of 1.03 µM. Topics: Antineoplastic Agents; Azoles; Bridged Bicyclo Compounds, Heterocyclic; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; Fluorouracil; Humans; Isoindoles; MCF-7 Cells; Neoplasms; Organoselenium Compounds; Thiadiazoles | 2015 |
Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy.
Thioredoxin reductase (TrxR) is critical for cellular redox regulation and is involved in tumor proliferation, apoptosis and metastasis. Its C-terminal redox-active center contains a cysteine (Cys497) and a unique selenocysteine (Sec498), which are exposed to solvent and easily accessible. Thus, it is becoming an important target for anticancer drugs. Selective inhibition of TrxR by 1,2-(bis-1,2-benzisoselenazol-3(2H)-one)ethane (4a) prevents proliferation of several cancer cell lines both in vivo and in vitro. Using the structure of 4a as a starting point, a series of novel bis-1,2-benzisoselenazol-3(2H)-ones was designed, prepared and tested to explore the structure-activity relationships (SARs) for this class of inhibitor and to improve their potency. Notably, 1,2-(5,5'-dimethoxybis(1,2-benzisoselenazol-3(2H)-one))ethane (12) was found to be more potent than 4a in both in vitro and in vivo evaluation. Its binding sites were confirmed by biotin-conjugated iodoacetamide assay and a SAR model was generated to guide further structural modification. Topics: Animals; Antineoplastic Agents; Cell Proliferation; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Humans; Liver; Models, Molecular; Molecular Structure; Neoplasms; Organoselenium Compounds; Rats; Stereoisomerism; Structure-Activity Relationship; Thioredoxin-Disulfide Reductase; Tumor Cells, Cultured | 2012 |