Compounds > 1-phthalidyl-5-fluorouracil
Page last updated: 2024-11-07

1-phthalidyl-5-fluorouracil

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

Description

1-phthalidyl-5-fluorouracil: prodrug of 5-fluorouracil; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID128467
CHEMBL ID21040
SCHEMBL ID4886494
MeSH IDM0128928

Synonyms (18)

Synonym
1-(1,3-dihydro-3-oxo-1-isobenzofuranyl)-5-fluoro-2,4(1h,3h)-pyrimidinedione
n(sub 1)-phthalidyl-5-fluorouracil
2,4(1h,3h)-pyrimidinedione, 1-(1,3-dihydro-3-oxo-1-isobenzofuranyl)-5-fluoro-
1-phthalidyl-5-fluorouracil
1-pfu
CHEMBL21040
81820-68-0
nf1jn84r8k ,
unii-nf1jn84r8k
SCHEMBL4886494
1-phthalidyl-5-fluorouracil, (+/-)-
n1-phthalidyl-5-fluorouracil
n-phthalidyl-5-fluorouracil
Q27284839
5-fluoro-4-hydroxy-1-(3-oxo-1,3-dihydro-2-benzofuran-1-yl)pyrimidin-2(1h)-one
DTXSID901002250
5-fluoro-1-(3-oxo-1,3-dihydroisobenzofuran-1-yl)pyrimidine-2,4(1h,3h)-dione
PD160058

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" The preclinical pharmacokinetic studies revealed a steep increase and rapid decrease of 590-S and activated 5-FU in the blood compared with those of other fluorinated pyrimidines."( [Pharmacokinetic studies of a new fluorinated pyrimidine, 590-S (PH-FU), in human patients].
, 1986)		0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID136585In vivo antitumor activity against MH 134 cell line in female BDF1 mice after oral administered dose of 25 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136584In vivo antitumor activity against MH 134 cell line in female BDF1 mice after oral administered dose of 200 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136592In vivo antitumor activity against P-388 Leukemia cell line in female BDF1 mice after oral administered dose of 200 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136589In vivo antitumor activity against Meth A cell line in female BDF1 mice after oral administered dose of 200 mg/kg; death1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136587In vivo antitumor activity against Meth A cell line in female BDF1 mice after oral administered dose of 150 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136583In vivo antitumor activity against MH 134 cell line in female BDF1 mice after oral administered dose of 150 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136593In vivo antitumor activity against P-388 Leukemia cell line in female BDF1 mice after oral administered dose of 25 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136594In vivo antitumor activity against P-388 Leukemia cell line in female BDF1 mice after oral administered dose of 50 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136590In vivo antitumor activity against Meth A cell line in female BDF1 mice after oral administered dose of 50 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136586In vivo antitumor activity against MH 134 cell line in female BDF1 mice after oral administered dose of 50 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136588In vivo antitumor activity against Meth A cell line in female BDF1 mice after oral administered dose of 200 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
AID136591In vivo antitumor activity against P-388 Leukemia cell line in female BDF1 mice after oral administered dose of 100 mg/kg1982Journal of medicinal chemistry, Oct, Volume: 25, Issue:10
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19909 (100.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)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: 12.15

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 Index12.15 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.15)

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%
Other9 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
3-methylcholanthrene
Methylcholanthrene: A carcinogen that is often used in experimental cancer studies.. 3-methylcholanthrene : A pentacyclic ortho- and peri-fused polycyclic arene consisting of a dihydrocyclopenta[ij]tetraphene ring system with a methyl substituent at the 3-position.		1.9710ortho- and peri-fused polycyclic arenearyl hydrocarbon receptor agonist;
carcinogenic agent
acetazolamide
Acetazolamide: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)		1.9610monocarboxylic acid amide;
sulfonamide;
thiadiazoles		anticonvulsant;
diuretic;
EC 4.2.1.1 (carbonic anhydrase) inhibitor
fluorouracil
Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.. 5-fluorouracil : A nucleobase analogue that is uracil in which the hydrogen at position 5 is replaced by fluorine. It is an antineoplastic agent which acts as an antimetabolite - following conversion to the active deoxynucleotide, it inhibits DNA synthesis (by blocking the conversion of deoxyuridylic acid to thymidylic acid by the cellular enzyme thymidylate synthetase) and so slows tumour growth.		3.4780nucleobase analogue;
organofluorine compound		antimetabolite;
antineoplastic agent;
environmental contaminant;
immunosuppressive agent;
radiosensitizing agent;
xenobiotic
phenobarbital
Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.		2.3720barbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
tegafur
[no description available]		1.9610organohalogen compound;
pyrimidines
ConditionIndicatedRelationship StrengthStudiesTrials
Leukemia P388
An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene.		01.9610
Experimental Neoplasms
[description not available]		02.6530
EHS Tumor
[description not available]		02.6630
Cancer of Colon
[description not available]		01.9710
Cancer of Stomach
[description not available]		02.6630
Colonic Neoplasms
Tumors or cancer of the COLON.		01.9710
Stomach Neoplasms
Tumors or cancer of the STOMACH.		02.6630
Breast Cancer
[description not available]		07.3720
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.3720
Experimental Hepatoma
[description not available]		02.3720
Cancer of Lung
[description not available]		01.9610
Reticulum Cell-Like Sarcoma, Yoshida
[description not available]		01.9610
Lung Neoplasms
Tumors or cancer of the LUNG.		01.9610
Experimental Leukemia
[description not available]		01.9610
Anorexia
The lack or loss of APPETITE accompanied by an aversion to food and the inability to eat. It is the defining characteristic of the disorder ANOREXIA NERVOSA.		01.9610
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		01.9610