10H-[1]benzothiolo[3,2-b]indole, also known as **benzothiopyranoindole**, is a heterocyclic compound with a fused ring system containing both benzene, thiophene, and indole moieties.
**Importance in Research:**
This compound and its derivatives have garnered significant interest in research due to their potential for diverse biological activities and therapeutic applications. Here's why:
* **Anti-cancer activity:** Studies have shown that benzothiopyranoindole derivatives exhibit promising anti-cancer activity against various cancer cell lines, including leukemia, breast cancer, and lung cancer. Their mechanism of action often involves inhibiting cell proliferation, inducing apoptosis, and affecting signaling pathways crucial for tumor growth.
* **Anti-inflammatory activity:** Some derivatives possess anti-inflammatory properties, potentially targeting inflammatory pathways like NF-κB. This makes them promising candidates for treating inflammatory diseases like arthritis and inflammatory bowel disease.
* **Antibacterial and antifungal activity:** Certain benzothiopyranoindoles display antibacterial and antifungal activities, potentially making them useful in developing new antimicrobial agents to combat resistant strains.
* **Neuroprotective activity:** Research indicates that some derivatives might possess neuroprotective effects, protecting against neuronal damage in conditions like Alzheimer's disease and Parkinson's disease.
* **Other potential applications:**
* **Anti-viral activity:** Studies are ongoing to evaluate their potential against viral infections.
* **Anti-parasitic activity:** Their effectiveness against parasitic infections is being explored.
* **Photodynamic therapy:** Some derivatives exhibit phototoxicity, making them promising candidates for photodynamic therapy, a non-invasive treatment method for cancer.
**Research Focus:**
Current research efforts primarily focus on:
* **Synthesis and structure-activity relationship (SAR) studies:** Researchers are exploring various synthetic methods to create new benzothiopyranoindole derivatives and investigating the relationship between their chemical structure and biological activity.
* **Mechanism of action studies:** Investigating the precise mechanisms by which these compounds exert their biological effects is crucial for understanding their potential as therapeutic agents.
* **Pharmacokinetic and toxicity studies:** Determining their pharmacokinetic properties (absorption, distribution, metabolism, and excretion) and potential toxicity profiles is vital for developing safe and effective drugs.
**Overall:** 10H-[1]benzothiolo[3,2-b]indole and its derivatives represent a promising class of compounds with diverse biological activities. Further research is ongoing to fully understand their potential for treating a wide range of diseases.
ID Source | ID |
---|---|
PubMed CID | 354261 |
CHEMBL ID | 1490022 |
CHEBI ID | 105992 |
SCHEMBL ID | 8654364 |
Synonym |
---|
nsc605333 |
nsc-605333 |
mls000757221 , |
10h-benzothiopheno[3,2-b]indole |
10h-[1]benzothieno[3,2-b]indole |
NCI60_004632 |
smr000529048 |
CHEBI:105992 |
10h-[1]benzothiolo[3,2-b]indole |
HMS2884F09 |
CHEMBL1490022 |
FPQLXWGSGNEDCF-UHFFFAOYSA-N |
SCHEMBL8654364 |
Q27183787 |
benzothieno[3,2-b]indole |
DTXSID201304576 |
248-67-9 |
10h-benzo[4,5]thieno[3,2-b]indole |
Class | Description |
---|---|
indoles | Any compound containing an indole skeleton. |
[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, Beta-lactamase | Escherichia coli K-12 | Potency | 89.1251 | 0.0447 | 17.8581 | 100.0000 | AID485294 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 13.4591 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
Nrf2 | Homo sapiens (human) | Potency | 12.5893 | 0.0920 | 8.2222 | 23.1093 | AID624171 |
glp-1 receptor, partial | Homo sapiens (human) | Potency | 28.1838 | 0.0184 | 6.8060 | 14.1254 | AID624417 |
chaperonin-containing TCP-1 beta subunit homolog | Homo sapiens (human) | Potency | 89.1251 | 3.9811 | 27.7649 | 39.8107 | AID504842 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 20.5878 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 18.3564 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
Microtubule-associated protein tau | Homo sapiens (human) | Potency | 6.2050 | 0.1800 | 13.5574 | 39.8107 | AID1460; AID1468 |
chromobox protein homolog 1 | Homo sapiens (human) | Potency | 100.0000 | 0.0060 | 26.1688 | 89.1251 | AID540317 |
parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 50.1187 | 3.5481 | 19.5427 | 44.6684 | AID743266 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 3.1623 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 79.4328 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
muscleblind-like protein 1 isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 0.0041 | 9.9625 | 28.1838 | AID2675 |
TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 1.7783 | 1.7783 | 16.2081 | 35.4813 | AID652104 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
RNA polymerase II cis-regulatory region sequence-specific DNA binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
DNA binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
double-stranded DNA binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
RNA binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
mRNA 3'-UTR binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
protein binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
lipid binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
identical protein binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
pre-mRNA intronic binding | TAR DNA-binding protein 43 | Homo sapiens (human) |
molecular condensate scaffold activity | TAR DNA-binding protein 43 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Process | via Protein(s) | Taxonomy |
---|---|---|
intracellular non-membrane-bounded organelle | TAR DNA-binding protein 43 | Homo sapiens (human) |
nucleus | TAR DNA-binding protein 43 | Homo sapiens (human) |
nucleoplasm | TAR DNA-binding protein 43 | Homo sapiens (human) |
perichromatin fibrils | TAR DNA-binding protein 43 | Homo sapiens (human) |
mitochondrion | TAR DNA-binding protein 43 | Homo sapiens (human) |
cytoplasmic stress granule | TAR DNA-binding protein 43 | Homo sapiens (human) |
nuclear speck | TAR DNA-binding protein 43 | Homo sapiens (human) |
interchromatin granule | TAR DNA-binding protein 43 | Homo sapiens (human) |
nucleoplasm | TAR DNA-binding protein 43 | Homo sapiens (human) |
chromatin | TAR DNA-binding protein 43 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
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. |
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 | |||
[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 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 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 (12.56) 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 | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |