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16-fluoroestradiol

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Description

16-fluoroestradiol is a synthetic analog of estradiol, the most potent natural estrogen. It has been studied for its potential use in treating breast cancer, as it exhibits antiproliferative activity against estrogen-dependent breast cancer cells. Its synthesis involves fluorination of the estradiol molecule at the 16-position, modifying its binding affinity to estrogen receptors. This modification alters its activity and pharmacodynamic properties, impacting its interaction with estrogen receptors. The compound is studied for its potential therapeutic applications in breast cancer treatment, as well as for understanding the role of estrogen signaling in various biological processes.'

16-fluoroestradiol: RN refers to (16beta,17beta)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID67101
CHEMBL ID1627847
SCHEMBL ID6543617
MeSH IDM0127837

Synonyms (10)

Synonym
16-fluoroestradiol
84693-92-5
CHEMBL1627847
estra-1,3,5(10)-triene-3,17-diol, 16-fluoro-, (16beta,17beta)-
16beta-fluoroestradiol
16alpha-(18)-fluoro-17beta-estradiol
f-18 16alpha-fluoroestradiol
SCHEMBL6543617
DTXSID101004983
16-fluoroestra-1(10),2,4-triene-3,17-diol
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (38)

Assay IDTitleYearJournalArticle
AID19785Tested in vivo for the biodistribution in rat muscle at 1 hour after intravenous dose of 120 microCi of the drug and 15 ug of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24388Tested in vivo for the biodistribution in rat bone after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19395Tested in vivo for the biodistribution in blood of female rat at 1 hour after intravenous dose of 120 microCi of the drug and 15 u g of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19602Tested in vivo for the biodistribution in rat kidney at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24236Partition coefficient (logP)1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID35537Relative binding affinity for Alphafetoprotein1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19791Tested in vivo for the biodistribution in rat ovaries after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID69676Relative binding affinity for estrogen receptor at 0C1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID16668Tested in vivo for the biodistribution in rat uterus at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19612Tested in vivo for the biodistribution in rat liver at 1 hour after intravenous dose of 120 microCi of the drug and 15 u g of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24579Tested in vivo for the biodistribution in rat muscle at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24574Tested in vivo for the biodistribution in rat liver after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24581Tested in vivo for the biodistribution in rat ovaries at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19816Tested in vivo for the biodistribution in rat uterus/blood after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID16657Tested in vivo for the biodistribution in rat uterus/muscle after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24582Tested in vivo for the biodistribution in rat ovaries at 1 hour after intravenous dose of 120 microCi of the drug and 15 ug of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID39321Relative binding affinity (RBA) against androgen receptor (AR) using [3H]R-1881 as competitive radioligand.1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Synthesis of high affinity fluorine-substituted ligands for the androgen receptor. Potential agents for imaging prostatic cancer by positron emission tomography.
AID227715Binding selectivity index (BSI) as the relative affinity for estrogen receptor at 25 degree C and no-specific binding1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24389Tested in vivo for the biodistribution in rat bone at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID69389Nonspecific binding affinity (NSB) for estrogen receptor1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19597Tested in vivo for the biodistribution in rat kidney after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID16663Tested in vivo for the biodistribution in rat uterus/muscle at 1 hour after intravenous dose of 120 microCi of the drug and 15 micro g of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24576Tested in vivo for the biodistribution in rat liver at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19394Tested in vivo for the biodistribution in blood of female rat at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24577Tested in vivo for the biodistribution in rat muscle after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24393Tested in vivo for the biodistribution in rat kidney at 1 hour after intravenous dose of 120 microCi of the drug and 15 u g of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19805Tested in vivo for the biodistribution in rat uterus after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19821Tested in vivo for the biodistribution in rat uterus/blood at 1 hour after intravenous dose of 120 microCi of the drug and 15 ug of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19586Tested in vivo for the biodistribution in rat fat after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19580Tested in vivo for the biodistribution in rat bone at 1 hour after intravenous dose of 120 microCi of the drug and 15 ug of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID16662Tested in vivo for the biodistribution in rat uterus/muscle at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24587Tested in vivo for the biodistribution in rat uterus/blood at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID24392Tested in vivo for the biodistribution in rat fat at 1 hour after intravenous dose of 120 microCi of the drug and 15 micro g of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID69677Relative binding affinity for estrogen receptor at 25 degree C1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID200434Relative binding affinity against sex steroid binding protein (SBP)1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19810Tested in vivo for the biodistribution in rat uterus at 1 hour after intravenous dose of 120 microCi of the drug and 15 micro g of estradiol1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19591Tested in vivo for the biodistribution in rat fat at 1 hour after intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
AID19389Tested in vivo for the biodistribution in blood of female rat after 3 hours following an intravenous dose of 120 microCi of drug in 10%ethanol saline1993Journal of medicinal chemistry, May-28, Volume: 36, Issue:11
16 beta-([18F]fluoro)estrogens: systematic investigation of a new series of fluorine-18-labeled estrogens as potential imaging agents for estrogen-receptor-positive breast tumors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (81)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (6.17)18.7374
1990's17 (20.99)18.2507
2000's17 (20.99)29.6817
2010's40 (49.38)24.3611
2020's2 (2.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.59

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 Index10.59 (24.57)
Research Supply Index4.52 (2.92)
Research Growth Index5.11 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.59)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (10.98%)5.53%
Reviews11 (13.41%)6.00%
Case Studies7 (8.54%)4.05%
Observational0 (0.00%)0.25%
Other55 (67.07%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]