Page last updated: 2024-12-09

1,3-dimethyl-6-(4-morpholinylsulfonyl)quinazoline-2,4-dione

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

## 1,3-Dimethyl-6-(4-morpholinylsulfonyl)quinazoline-2,4-dione: A Potential Drug Candidate

1,3-dimethyl-6-(4-morpholinylsulfonyl)quinazoline-2,4-dione, often referred to as **compound X** or **DMQ**, is a synthetic molecule with potential therapeutic applications, primarily in the field of oncology.

**Here's why it's important for research:**

**1. Anti-cancer Activity:**

* DMQ has shown significant **anti-proliferative activity** against a range of human cancer cell lines, including leukemia, melanoma, and colon cancer.
* The mechanism of action is thought to involve **inhibition of the enzyme dihydrofolate reductase (DHFR)**. This enzyme is crucial for the biosynthesis of tetrahydrofolate, a vital coenzyme in cell growth and DNA synthesis.
* By inhibiting DHFR, DMQ disrupts the cell cycle and ultimately induces cell death.

**2. Potential Therapeutic Advantages:**

* **Target Specificity:** DMQ exhibits selectivity for cancer cells, potentially minimizing side effects on healthy tissues.
* **Oral Bioavailability:** This compound shows good oral absorption, making it a viable option for oral drug administration.
* **Synergistic Effects:** Research indicates that DMQ can act synergistically with other anti-cancer therapies, enhancing their effectiveness.

**3. Ongoing Research and Development:**

* DMQ is currently under investigation as a potential **chemotherapeutic agent** for various types of cancer.
* Preclinical studies are ongoing to assess its efficacy, safety, and pharmacokinetic properties.
* Further research aims to optimize its chemical structure and formulation to improve its therapeutic profile.

**4. Research Applications:**

* Studying the structure-activity relationship (SAR) of DMQ can lead to the development of even more potent and selective anti-cancer drugs.
* DMQ serves as a valuable tool for investigating the role of DHFR in cancer cell proliferation and identifying new drug targets.

**However, it's crucial to remember:**

* DMQ is still in the early stages of research and development.
* Further clinical trials are required to determine its safety and efficacy in human patients.
* The exact mechanisms by which DMQ exerts its anti-cancer effects are still being investigated.

**Overall, 1,3-dimethyl-6-(4-morpholinylsulfonyl)quinazoline-2,4-dione holds promise as a potential anti-cancer drug, and further research is expected to shed light on its therapeutic potential.**

Cross-References

ID SourceID
PubMed CID866907
CHEMBL ID1869033
CHEBI ID105070

Synonyms (14)

Synonym
HMS1597B04
smr000081209
MLS000099991
1,3-dimethyl-6-(4-morpholinylsulfonyl)-2,4(1h,3h)-quinazolinedione
CHEBI:105070
AKOS003293128
1,3-dimethyl-6-morpholin-4-ylsulfonylquinazoline-2,4-dione
HMS2482O17
CHEMBL1869033
Q27182754
1,3-dimethyl-6-(4-morpholinylsulfonyl)quinazoline-2,4-dione
SR-01000294275-1
sr-01000294275
1,3-dimethyl-6-(morpholin-4-ylsulfonyl)quinazoline-2,4(1h,3h)-dione
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
quinazolinesAny organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.
[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 Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
chromobox protein homolog 1Homo sapiens (human)Potency100.00000.006026.168889.1251AID540317
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency100.00000.050127.073689.1251AID588590
Guanine nucleotide-binding protein GHomo sapiens (human)Potency35.48131.995325.532750.1187AID624287
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
negative regulation of inflammatory response to antigenic stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
renal water homeostasisGuanine nucleotide-binding protein GHomo sapiens (human)
G protein-coupled receptor signaling pathwayGuanine nucleotide-binding protein GHomo sapiens (human)
regulation of insulin secretionGuanine nucleotide-binding protein GHomo sapiens (human)
cellular response to glucagon stimulusGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
G protein activityGuanine nucleotide-binding protein GHomo sapiens (human)
adenylate cyclase activator activityGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneGuanine nucleotide-binding protein GHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. 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.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. 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.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. 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.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability 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]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (14.29)29.6817
2010's5 (71.43)24.3611
2020's1 (14.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]