(1,2-bis(1,2-benzisoselenazolone-3(2H)-ketone))ethane: has antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 10387485 |
| CHEMBL ID | 2035460 |
| SCHEMBL ID | 3561403 |
| MeSH ID | M0455226 |
| Synonym |
|---|
| (1,2-bis(1,2-benzisoselenazolone-3(2h)-ketone))ethane |
| ethaselen |
| us8592468, ebse14 |
| bdbm50385303 |
| compound eb |
| ethaselen-1 |
| bbske |
| shuang-xi-zuo-wan-1 |
| CHEMBL2035460 , |
| SCHEMBL3561403 |
| unii-4q2ezs1iwg |
| 2,2'-(1,2-ethanediyl)bis(1,2-benzisoselenazol-3(2h)-one) |
| 217798-39-5 |
| 1,2-benzisoselenazol-3(2h)-one, 2,2'-(1,2-ethanediyl)bis- |
| 4q2ezs1iwg , |
| DB15051 |
| 2-[2-(3-oxo-1,2-benzoselenazol-2-yl)ethyl]-1,2-benzoselenazol-3-one |
| 2,2'-(ethane-1,2-diyl)bis(benzo[d][1,2]selenazol-3(2h)-one) . |
| EX-A5107 |
| HY-116749 |
| CS-0066457 |
| AKOS040757392 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The method was successfully applied to the pharmacokinetic study in dogs." | ( High performance liquid chromatographic determination of 1,2-[bis(1,2-benzisoselenazolone-3(2H)-ketone)]-ethane (BBSKE), a novel organoselenium compound, in dog plasma using pre-column derivatization and its application in pharmacokinetic study. Dou, GF; Lou, YQ; Meng, ZY; Zhang, GL; Zhou, HY, 2007) | 0.34 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Twenty-four mice were injected intraperitoneally with single cell suspension of TRAMP-C2 cell and then divided into 3 groups of 8 mice undergoing intraperitoneal injection for 7 days: BBSKE group (BBSKE was administered at the dosage of 25mg/kg/day), cisplatin group (cisplatin 2mg/kg/d was injected), and control group (pure solvent was injected)." | ( [Induction of apoptosis in prostate cancer cell line PC-3 by BBSKE, a novel organoselenium compound, and its effect in vivo]. Li, HW; Shi, CJ; Wu, XQ; Yang, FG; Yu, LZ; Zeng, HH, 2003) | 0.32 |
| " After exposure of PC-3 cells to BBSKE at the dosage of 20 micro mol/L for 48 hours the apoptosis rate was 26." | ( [Induction of apoptosis in prostate cancer cell line PC-3 by BBSKE, a novel organoselenium compound, and its effect in vivo]. Li, HW; Shi, CJ; Wu, XQ; Yang, FG; Yu, LZ; Zeng, HH, 2003) | 0.32 |
| " Compared with selenite single treatment, dosage of selenite could be remarkably reduced in combination therapy to gain the same inhibitory effect on cell proliferation." | ( Synergistic effect of ethaselen and selenite treatment against A549 human non-small cell lung cancer cells. Ma, WW; Xu, W; Zeng, HH, 2014) | 0.4 |
| "All these results indicate that the combination treatment of BBSKE and selenite showed synergism to inhibit A549 cell proliferation in vitro, and also reduced the selenite dosage to mitigate its toxicity which is very meaningful for combination chemotherapy of lung cancer." | ( Synergistic effect of ethaselen and selenite treatment against A549 human non-small cell lung cancer cells. Ma, WW; Xu, W; Zeng, HH, 2014) | 0.4 |
| " In this study, we combined an organic selenium compound--TrxR inhibitor ethaselen (BBSKE) with low dosage sodium selenite to inhibit proliferation and induce death of NSCLC cells, and identified underlying mechanisms." | ( Synergism between thioredoxin reductase inhibitor ethaselen and sodium selenite in inhibiting proliferation and inducing death of human non-small cell lung cancer cells. Dong, C; Sun, R; Xu, W; Yin, H; Zeng, H; Zheng, X, 2017) | 0.46 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Thioredoxin reductase 1, cytoplasmic | Rattus norvegicus (Norway rat) | IC50 (µMol) | 6.0000 | 0.2720 | 1.8260 | 6.0000 | AID665488 |
| Thioredoxin reductase 1, cytoplasmic | Homo sapiens (human) | IC50 (µMol) | 5.0000 | 0.0432 | 2.2655 | 5.0000 | AID665478 |
| Thioredoxin reductase 3 | Homo sapiens (human) | IC50 (µMol) | 5.0000 | 0.3500 | 3.1167 | 5.0000 | AID665478 |
| Thioredoxin reductase 2, mitochondrial | Homo sapiens (human) | IC50 (µMol) | 5.0000 | 0.3500 | 3.1167 | 5.0000 | AID665478 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1406795 | Antiproliferative activity against human BEAS2B cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1275496 | Antiproliferative activity against human HeLa cells after 48 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Synthesis and antiproliferative evaluation of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold. |
| AID665490 | Inhibition of human glutathione reductase Sec498Cys mutant at 100 uM after 10 mins by GSSH reduction assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID1406790 | Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1406792 | Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1275495 | Antiproliferative activity against human SMMC7721 cells after 48 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Synthesis and antiproliferative evaluation of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold. |
| AID665483 | Inhibition of human glutathione reductase at 100 uM after 10 mins by GSSH reduction assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID665474 | Inhibition of TrxR1 in rat liver homogenate preincubated for 5 mins measured by DNTB assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID1406793 | Antiproliferative activity against human 184B5 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1887896 | Antitumor activity against human MHCC97H cells xenografted in BALB/c mouse assessed as tumor volume at 30 mg/kg, ip administered every other day for 30 days | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR. |
| AID1406797 | Selectivity index, ratio of GI50 for human BEAS2B cells to GI50 for human HTB-54 cells | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1406794 | Antiproliferative activity against human HTB-54 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1406791 | Antiproliferative activity against human CCRF-CEM cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1406789 | Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1275497 | Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Synthesis and antiproliferative evaluation of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold. |
| AID665489 | Inhibition of human C-terminal truncated TrxR | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID1275498 | Antiproliferative activity against mouse L929 cells after 48 hrs by CCK8 assay | 2016 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 26, Issue:4 | Synthesis and antiproliferative evaluation of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold. |
| AID1887892 | Antitumor activity against human MHCC97H cells xenografted in BALB/c mouse assessed as tumor growth inhibition at 30 mg/kg, ip administered every other day for 30 days | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR. |
| AID665478 | Inhibition of TrxR in human U87MG cells after 12 hrs by insulin-reducing method | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID665475 | Growth inhibition of human MIAPaCa2 cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID665477 | Growth inhibition of human LoVo cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID665476 | Growth inhibition of human U87MG cells after 48 hrs by MTT assay | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID665488 | Non-competitive inhibition of rat TrxR1 | 2012 | Bioorganic & medicinal chemistry, Jun-15, Volume: 20, Issue:12 | Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapy. |
| AID1406796 | Selectivity index, ratio of GI50 for human 184B5 cells to GI50 for human MCF7 cells | 2018 | European journal of medicinal chemistry, Sep-05, Volume: 157 | Novel selenadiazole derivatives as selective antitumor and radical scavenging agents. |
| AID1887895 | Antitumor activity against human MHCC97H cells xenografted in BALB/c mouse assessed as tumor weight at 30 mg/kg, ip administered every other day for 30 days | 2022 | European journal of medicinal chemistry, Jan-05, Volume: 227 | Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 10 (34.48) | 29.6817 |
| 2010's | 17 (58.62) | 24.3611 |
| 2020's | 2 (6.90) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (11.17) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 29 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||