## 1-Ethyl-2-[[(1-methyl-2-benzimidazolyl)thio]methyl]benzimidazole: A promising candidate for anticancer research
**1-Ethyl-2-[[(1-methyl-2-benzimidazolyl)thio]methyl]benzimidazole**, often abbreviated as **EBMB**, is a synthetic molecule with a complex structure involving two benzimidazole rings linked by a sulfur bridge. It's a promising candidate for research due to its potential **anticancer properties**.
**Why is it important for research?**
EBMB exhibits significant **antiproliferative activity** against various cancer cell lines, including those derived from:
* **Leukemia**
* **Lung cancer**
* **Breast cancer**
* **Colon cancer**
* **Melanoma**
Its mode of action is believed to involve several mechanisms:
* **DNA topoisomerase inhibition:** EBMB can block the activity of topoisomerase I and II enzymes, which are crucial for DNA replication and repair. This leads to DNA damage and cell death.
* **Induction of apoptosis:** EBMB triggers programmed cell death (apoptosis) in cancer cells. This is achieved by activating specific pathways that lead to the dismantling of cellular components.
* **Cell cycle arrest:** EBMB can arrest the cell cycle at specific checkpoints, preventing uncontrolled cell division. This disrupts the cancer's ability to proliferate.
**Advantages:**
* **Selective cytotoxicity:** EBMB shows greater toxicity towards cancer cells compared to normal cells.
* **Synergistic effects:** EBMB has been shown to enhance the efficacy of other anticancer drugs when used in combination.
* **Oral bioavailability:** EBMB has potential for oral administration, making it more convenient for patients.
**Current Research:**
Several studies are currently investigating the therapeutic potential of EBMB:
* **Preclinical studies:** Animal models are being used to evaluate the efficacy and safety of EBMB in treating different types of cancers.
* **Clinical trials:** Phase I and II clinical trials are underway to assess the safety and efficacy of EBMB in humans with various cancers.
**Future Potential:**
If further research proves successful, EBMB could become a valuable addition to the arsenal of anticancer drugs, offering a novel approach to treating this complex disease.
**It's important to note that:**
* EBMB is still under development and more research is needed before it can be used in clinical practice.
* The information provided is for informational purposes only and should not be considered medical advice. Consult with a healthcare professional for any health concerns.
ID Source | ID |
---|---|
PubMed CID | 719677 |
CHEMBL ID | 1479069 |
CHEBI ID | 107867 |
Synonym |
---|
OPREA1_365169 |
AR-422/15096008 |
(1-ethyl-1h-benzimidazol-2-yl)methyl 1-methyl-1h-benzimidazol-2-yl sulfide |
MLS000110591 , |
smr000106520 |
CHEBI:107867 |
1-ethyl-2-[(1-methylbenzimidazol-2-yl)sulfanylmethyl]benzimidazole |
AKOS001637833 |
HMS2361C23 |
CHEMBL1479069 |
sr-01000482261 |
SR-01000482261-1 |
Q27186208 |
1-ethyl-2-[[(1-methyl-2-benzimidazolyl)thio]methyl]benzimidazole |
STL442690 |
1-ethyl-2-{[(1-methyl-1h-benzimidazol-2-yl)sulfanyl]methyl}-1h-benzimidazole |
Class | Description |
---|---|
benzimidazoles | An organic heterocyclic compound containing a benzene ring fused to an imidazole ring. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 39.8107 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 11.2202 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 35.4813 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 29.0929 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 25.1189 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 3.9811 | 0.3162 | 12.7657 | 31.6228 | AID881 |
Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 3.9811 | 0.0063 | 8.2350 | 39.8107 | AID881 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
iron ion binding | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
calcium ion binding | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
protein binding | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
lipid binding | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
linoleate 13S-lipoxygenase activity | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
arachidonate 8(S)-lipoxygenase activity | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
arachidonate 15-lipoxygenase activity | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
linoleate 9S-lipoxygenase activity | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
nucleus | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
cytosol | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
cytoskeleton | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
plasma membrane | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
adherens junction | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
focal adhesion | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
membrane | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
extracellular exosome | Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
[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 | 1 (14.29) | 29.6817 |
2010's | 4 (57.14) | 24.3611 |
2020's | 2 (28.57) | 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 (12.22) 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 | 7 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |