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1-(4,6-dimethoxypyrimidin-2-yl)-3-(2-ethoxyphenoxysulfonyl)urea

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

Description

You're asking about **1-(4,6-dimethoxypyrimidin-2-yl)-3-(2-ethoxyphenoxysulfonyl)urea**, also known as **Lestaurtinib**. It's a drug that has been studied extensively in research for its potential to treat various diseases.

Here's why it's important for research:

* **Kinase Inhibitor:** Lestaurtinib is a potent inhibitor of several protein kinases, particularly **FLT3**. FLT3 is a receptor tyrosine kinase involved in the growth and development of blood cells. Mutations in the FLT3 gene are found in a significant number of patients with acute myeloid leukemia (AML), a type of cancer affecting the blood and bone marrow.
* **Potential Anti-Cancer Drug:** Due to its ability to block FLT3 signaling, Lestaurtinib has shown promise in clinical trials as a treatment for **FLT3-mutated AML**. It has also been investigated for other hematological malignancies and solid tumors.
* **Target Validation:** The research surrounding Lestaurtinib has helped to validate FLT3 as a promising therapeutic target for cancer treatment.
* **Mechanism of Action Studies:** Research with Lestaurtinib has contributed to a better understanding of how kinase inhibitors work at a molecular level. This knowledge can help guide the development of future drugs that target these pathways.

**Important Notes:**

* **Clinical Development:** While Lestaurtinib has shown promise in early clinical trials, it has not yet received approval from the FDA for widespread use.
* **Side Effects:** Like all medications, Lestaurtinib can have side effects. Research is ongoing to optimize its safety and efficacy.
* **Ongoing Research:** Lestaurtinib continues to be investigated in clinical trials for various cancer types and other diseases, including solid tumors and autoimmune disorders.

**In summary, 1-(4,6-dimethoxypyrimidin-2-yl)-3-(2-ethoxyphenoxysulfonyl)urea (Lestaurtinib) is a significant molecule in drug discovery and research because of its potential to treat cancers, particularly those with FLT3 mutations.**

1-(4,6-dimethoxypyrimidin-2-yl)-3-(2-ethoxyphenoxysulfonyl)urea: herbicide; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3623881
CHEMBL ID2313153
CHEBI ID81748
SCHEMBL ID65311
MeSH IDM0539909

Synonyms (36)

Synonym
126801-58-9
ethoxysulfuron
A805606
(2-ethoxyphenyl) n-[(4,6-dimethoxypyrimidin-2-yl)carbamoyl]sulfamate
unii-2a9c8090zd
ethoxysulfuron [iso]
2a9c8090zd ,
C18440
sulfamic acid, [[(4,6-dimethoxy-2-pyrimidinyl)amino]carbonyl](2-ethoxyphenyl)-
FT-0631123
AKOS015895277
CHEMBL2313153 ,
bdbm50424592
chebi:81748 ,
SCHEMBL65311
hoe-095404
3-(4,6-dimethoxypyrimidin-2-yl)-1-(2-ethoxyphenoxysulfonylurea)
n-(((4,6-dimethoxy-2-pyrimidinyl)amino)carbonyl)sulfamic acid 2-ethoxyphenyl ester
2-ethoxyphenyl (((4,6-dimethoxy-2-pyrimidinyl)amino)carbonyl)sulfamate
1-(4,6-dimethoxypyrimidin-2-yl)-3-(2-ethoxyphenoxysulfonyl)urea
ethoxysulfuron [mi]
DTXSID1057951
1-(2-ethoxyphenoxysulfonyl)-3-(4,6-dimethoxy-2-pyrimidyl)urea
1-(2-ethoxyphenoxysulfonyl)-3-(4,6-dimethoxy-2-pyrimidyl)-urea
n'-(4,6-dimethoxypyrimidin-2-yl)-n-(2-ethoxyphenoxysulfonyl)urea
3-(4,6-dimethoxypyrimidin-2-yl)-1-(2-ethoxyphenoxysulfonyl)urea
2-ethoxyphenyl [(4,6-dimethoxy-2-pyrimidinyl)carbamoyl]sulfamate
J-005438
ethoxysulfuron, pestanal(r), analytical standard
2-ethoxyphenyl 4,6-dimethoxypyrimidin-2-ylcarbamoylsulfamate
Q22807473
ethoxysulfuron 100 microg/ml in acetonitrile
sulfamic acid, n-[[(4,6-dimethoxy-2-pyrimidinyl)amino]carbonyl]-, 2-ethoxyphenyl ester
D92859
AS-76182
n-[[(4,6-dimethoxy-2-pyrimidinyl)amino]carbonyl]sulfamic acid, 2-ethoxyphenyl ester
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
[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 (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Acetolactate synthase catalytic subunit, mitochondrialSaccharomyces cerevisiae S288CKi0.06400.00330.12840.4000AID721536
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID1585636Antifungal activity against Saccharomyces cerevisiae SC XH1549 cultured in YNB media after 48 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1585634Antifungal activity against fluconazole-resistant Candida albicans isolate g5 cultured in YNB media after 72 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1585628Antifungal activity against Candida albicans SC5314 cultured in YNB media after 72 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1592344Antifungal activity against Candida albicans isolate 17 grown in RPMI 1640 medium incubated for 24 hrs by microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives.
AID1585624Antifungal activity against Candida albicans SC5314 cultured in RPMI 1640 media after 24 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1585638Antifungal activity against Candida parapsilosis ATCC 22019 cultured in YNB media after 24 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID721544Antifungal activity against Candida albicans after 72 hrs by disk diffusion method2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Sulfonylureas have antifungal activity and are potent inhibitors of Candida albicans acetohydroxyacid synthase.
AID1585621Inhibition of Candida albicans AHAS catalytic subunit using pyruvate as substrate measured after 30 mins by colorimetric method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1592349Antifungal activity against Candida albicans isolate g5 grown in RPMI 1640 medium incubated for 24 hrs by microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives.
AID1585629Antifungal activity against fluconazole-resistant Candida albicans isolate 17 cultured in YNB media after 24 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID721535Inhibition of Candida albicans acetohydroxyacid synthase catalytic domain expressed in Escherichia coli by colorimetric method2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Sulfonylureas have antifungal activity and are potent inhibitors of Candida albicans acetohydroxyacid synthase.
AID721539Antifungal activity against Saccharomyces cerevisiae after 72 hrs by broth microdilution assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Sulfonylureas have antifungal activity and are potent inhibitors of Candida albicans acetohydroxyacid synthase.
AID1585625Antifungal activity against Candida albicans SC5314 cultured in YNB media after 24 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1592350Antifungal activity against Candida albicans SC5314 grown in YNB medium incubated for 24 hrs by microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives.
AID1585623Antifungal activity against Candida albicans SC5314 infected in Caenorhabditis elegans assessed as mortality at 20 nM after 24 hrs by propidium iodide staining based fluorescence microscopic analysis (Rvb = 17%)2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID721536Inhibition of Saccharomyces cerevisiae acetohydroxyacid synthase by colorimetric assay2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Sulfonylureas have antifungal activity and are potent inhibitors of Candida albicans acetohydroxyacid synthase.
AID1585639Antifungal activity against Candida parapsilosis ATCC 22019 cultured in YNB media after 48 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1592352Antifungal activity against Candida albicans isolate g5 grown in YNB medium incubated for 24 hrs by microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives.
AID1585640Antifungal activity against Candida parapsilosis ATCC 22019 cultured in YNB media after 72 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1585627Antifungal activity against Candida albicans SC5314 cultured in YNB media after 48 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1585630Antifungal activity against fluconazole-resistant Candida albicans isolate 17 cultured in YNB media after 48 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID721538Antifungal activity against Candida albicans after 72 hrs by broth microdilution method2013Journal of medicinal chemistry, Jan-10, Volume: 56, Issue:1
Sulfonylureas have antifungal activity and are potent inhibitors of Candida albicans acetohydroxyacid synthase.
AID1585633Antifungal activity against fluconazole-resistant Candida albicans isolate g5 cultured in YNB media after 48 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1585635Antifungal activity against Saccharomyces cerevisiae SC XH1549 cultured in YNB media after 24 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1592351Antifungal activity against Candida albicans isolate 17 grown in YNB medium incubated for 24 hrs by microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives.
AID1592346Antifungal activity against Candida albicans SC5314 grown in RPMI 1640 medium incubated for 24 hrs by microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives.
AID1585631Antifungal activity against fluconazole-resistant Candida albicans isolate 17 cultured in YNB media after 72 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1585637Antifungal activity against Saccharomyces cerevisiae SC XH1549 cultured in YNB media after 72 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1592347Inhibition of Candida albicans AHAS catalytic subunit at 10 uM using pyruvate as substrate measured after 30 mins by colorimetric method relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives.
AID1585632Antifungal activity against fluconazole-resistant Candida albicans isolate g5 cultured in YNB media after 24 hrs by broth microdilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Chemical preparation, biological evaluation and 3D-QSAR of ethoxysulfuron derivatives as novel antifungal agents targeting acetohydroxyacid synthase.
AID1592348Inhibition of Candida albicans AHAS catalytic subunit at 100 uM using pyruvate as substrate measured after 30 mins by colorimetric method relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Chemical synthesis, crystal structure, versatile evaluation of their biological activities and molecular simulations of novel pyrithiobac derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (16.67)29.6817
2010's5 (83.33)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.26

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.

MetricThis Compound (vs All)
Research Demand Index13.26 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index5.21 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.26)

All Compounds (24.57)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]