## 1-Methoxy-10H-acridin-9-one: A Promising Anti-Cancer Agent
1-Methoxy-10H-acridin-9-one, often simply called **methoxyacridone**, is a synthetic organic compound with a chemical formula of C₁₄H₁₁NO₃. Its structure features a 9-acridone core with a methoxy group attached at the 1-position.
**Why is it important for research?**
Methoxyacridone has shown significant potential as an **anti-cancer agent** due to its various biological activities, including:
* **DNA intercalation:** Methoxyacridone binds strongly to DNA, disrupting its function and potentially inhibiting cell growth and division. This mechanism is similar to how some chemotherapeutic drugs work.
* **Topoisomerase inhibition:** It can block the action of topoisomerases, enzymes crucial for DNA replication and repair. This further hinders cell proliferation.
* **Induction of apoptosis:** Methoxyacridone can trigger programmed cell death (apoptosis) in cancer cells, leading to their elimination.
* **Anti-angiogenic properties:** It can inhibit the formation of new blood vessels (angiogenesis) that are essential for tumor growth and spread.
* **Anti-inflammatory effects:** Methoxyacridone has been shown to reduce inflammation, which can play a role in cancer development and progression.
**Current Research:**
Methoxyacridone is currently undergoing preclinical studies to evaluate its efficacy and safety in treating different types of cancer, including:
* **Breast cancer:** Preclinical studies indicate that methoxyacridone shows promising activity against breast cancer cells, both in vitro and in vivo.
* **Lung cancer:** Research suggests that methoxyacridone can inhibit the growth of lung cancer cells and reduce tumor size in animal models.
* **Leukemia:** Studies are ongoing to investigate the potential of methoxyacridone in treating various types of leukemia.
**Future Directions:**
While methoxyacridone holds promise as a potential anti-cancer drug, further research is needed to:
* **Optimize its pharmacological properties:** Researchers are exploring ways to improve its solubility, bioavailability, and stability to enhance its effectiveness.
* **Develop safe and effective delivery systems:** Finding optimal ways to deliver methoxyacridone to the target cells is crucial for its clinical application.
* **Conduct clinical trials:** Extensive clinical trials are required to evaluate its safety, efficacy, and optimal dosage in humans.
**Conclusion:**
1-Methoxy-10H-acridin-9-one is a promising anti-cancer agent with multiple modes of action. Continued research efforts are essential to translate its preclinical potential into effective cancer therapies for patients.
ID Source | ID |
---|---|
PubMed CID | 409920 |
CHEMBL ID | 243813 |
CHEBI ID | 119975 |
SCHEMBL ID | 9352467 |
Synonym |
---|
nsc25171 |
nsc-25171 |
6950-01-2 |
1-methoxy-9(10h)-acridinone |
MLS001178926 |
smr000477711 |
AP-782/41885433 |
rd6-5070 |
1-methoxy-10-hydroacridin-9-one |
1-methoxy-10h-acridin-9-one |
CHEBI:119975 |
CHEMBL243813 , |
bdbm50371106 |
HMS2822G08 |
SCHEMBL9352467 |
Q27207760 |
DTXSID50328403 |
methoxyacridone |
Class | Description |
---|---|
acridines | |
[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 | 31.6228 | 5.6234 | 17.2929 | 31.6228 | AID485281 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 16.9441 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 84.2789 | 0.1000 | 20.8793 | 79.4328 | AID588453; AID588456 |
TDP1 protein | Homo sapiens (human) | Potency | 18.3564 | 0.0008 | 11.3822 | 44.6684 | AID686978 |
nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.0000 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
glucocerebrosidase | Homo sapiens (human) | Potency | 22.3872 | 0.0126 | 8.1569 | 44.6684 | AID2101 |
P53 | Homo sapiens (human) | Potency | 79.4328 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 5.8048 | 36.1306 | 65.1308 | AID540253 |
snurportin-1 | Homo sapiens (human) | Potency | 39.8107 | 5.8048 | 36.1306 | 65.1308 | AID540253 |
GTP-binding nuclear protein Ran isoform 1 | Homo sapiens (human) | Potency | 39.8107 | 5.8048 | 16.9962 | 25.9290 | AID540253 |
DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 89.1251 | 0.1000 | 28.9256 | 213.3130 | AID588591 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 3.1623 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
geminin | Homo sapiens (human) | Potency | 29.0929 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
Alpha-synuclein | Homo sapiens (human) | Potency | 25.1189 | 0.5623 | 9.3985 | 25.1189 | AID652106 |
Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 50.1187 | 1.9953 | 25.5327 | 50.1187 | AID624287 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Broad substrate specificity ATP-binding cassette transporter ABCG2 | Homo sapiens (human) | IC50 (µMol) | 6.3000 | 0.0040 | 1.9666 | 10.0000 | AID294540 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
AID494204 | Antiproliferative activity against human HaCaT cells after 48 hrs by phase contrast microscopy | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Structure-activity relationship studies of acridones as potential antipsoriatic agents. 1. Synthesis and antiproliferative activity of simple N-unsubstituted 10H-acridin-9-ones against human keratinocyte growth. |
AID494205 | Antiproliferative activity against human HaCaT cells assessed as LDH release at 2 uM after 48 hrs by phase contrast microscopy | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Structure-activity relationship studies of acridones as potential antipsoriatic agents. 1. Synthesis and antiproliferative activity of simple N-unsubstituted 10H-acridin-9-ones against human keratinocyte growth. |
AID494206 | Antioxidant activity assessed as DPPH free radical scavenging activity after 30 mins | 2010 | European journal of medicinal chemistry, Aug, Volume: 45, Issue:8 | Structure-activity relationship studies of acridones as potential antipsoriatic agents. 1. Synthesis and antiproliferative activity of simple N-unsubstituted 10H-acridin-9-ones against human keratinocyte growth. |
AID294541 | Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry relative to GF120918 | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Acridone derivatives: design, synthesis, and inhibition of breast cancer resistance protein ABCG2. |
AID294540 | Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry | 2007 | Bioorganic & medicinal chemistry, Apr-15, Volume: 15, Issue:8 | Acridone derivatives: design, synthesis, and inhibition of breast cancer resistance protein ABCG2. |
[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 | 2 (28.57) | 29.6817 |
2010's | 4 (57.14) | 24.3611 |
2020's | 1 (14.29) | 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 (12.28) 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] |