Page last updated: 2024-12-06

sulofenur

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

Description

sulofenur: a diarylsulfonylurea [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60417
CHEMBL ID7643
SCHEMBL ID4174
MeSH IDM0162382

Synonyms (44)

Synonym
NCI60_019612
NCI60_014449
ly-186641
n-(4-chlorophenylaminocarbonyl)indane-5-sulfonamide
n-(5-indansulfonyl)-n'-(4-chlorophenyl)urea
ly 186641
ly186641
1-(p-chlorophenyl)-3-(5-indanylsulfonyl)urea
1h-indene-5-sulfonamide, n-(((4-chlorophenyl)amino)carbonyl)-2,3-dihydro-
1h-indene-5-sulfonamide, 2,3-dihydro-n-(((4-chlorophenyl)amino)carbonyl)-
sulofenurum [inn-latin]
brn 4205979
nsc-642684
nsc642684
nsc-645012
nsc656667
sulofenur
nsc-656667
nsc645012
1-(4-chlorophenyl)-3-indan-5-ylsulfonyl-urea
n-(indanyl-5-sulfonyl)-n'-(4-chlorophenyl)urea
110311-27-8
sulofenur (usan/inn)
D05968
1-(4-chlorophenyl)-3-(2,3-dihydro-1h-inden-5-ylsulfonyl)urea
CHEMBL7643
unii-z45n070n3s
sulofenurum
z45n070n3s ,
sulofenur [usan:inn:ban]
SCHEMBL4174
sulofenur [mart.]
sulofenur [usan]
sulofenur [inn]
n-[[(4-chlorophenyl)amino]carbonyl]-indan-5-sulfonamide
n-([(4-chlorophenyl)amino]carbonyl)-2,3-dihydro-1h-indene-5-sulfonamide
JQJSFAJISYZPER-UHFFFAOYSA-N
nsc 642684; nsc 645012; nsc 656667
DTXSID20149208
BCP23826
ly186641; ly-186641; ly 186641
n-((4-chlorophenyl)carbamoyl)-2,3-dihydro-1h-indene-5-sulfonamide
oleylmyristate
Q27294971

Research Excerpts

Overview

Sulofenur is a novel diarylsulfonylurea with proven anti-tumor activity in murine tumor models. It is being tested in patients with advanced epithelial ovarian cancer refractory to standard chemotherapy.

ExcerptReferenceRelevance
"Sulofenur is a member of a new class of antineoplastic agents with a novel chemical structure and unique pharmacological and biological properties. "( Phase II study of sulofenur (LY 186641). A novel antineoplastic agent in advanced non-small cell lung cancer.
Einhorn, LH; Fossella, F; Lippman, SM; Munshi, NC; Seitz, DE, 1993
)
2.06
"Sulofenur is a novel diarylsulfonylurea with proven anti-tumor activity in murine tumor models. "( A phase II study of sulofenur (LY186641) in gastric cancer.
Coleman, R; Hatty, S; Kamthan, A; Peters, B; Scarffe, JH; Smyth, JF; Walling, J, 1992
)
2.05
"Sulofenur is a diarylsulfonylurea with demonstrated antitumor activity in patients with advanced epithelial ovarian cancer refractory to standard chemotherapy. "( Antitumor activity and clinical pharmacology of sulofenur in ovarian cancer.
Alberts, DS; Grindey, GB; Hamilton, M; Matzner, M; McCloskey, TM; Peng, YM; Plezia, PM; Roe, DJ; Seitz, D; Taylor, CW, 1992
)
1.98

Effects

ExcerptReferenceRelevance
"Sulofenur has been evaluated in phase I and II trials in adults with a variety of solid tumors, but the toxicity and maximum tolerated dose of sulofenur in children and adolescents have not been determined."( A phase I study of sulofenur in refractory pediatric malignant solid tumors.
Avery, L; Bowman, LC; Luo, X; Marina, N; Meyer, WH; Pappo, A; Pratt, CB, 1995
)
1.34

Treatment

ExcerptReferenceRelevance
"Sulofenur treatment (12.5 microM-1 mM) of colon adenocarcinoma cell lines resulted in dose- and time-dependent cell killing. "( Sulofenur cytotoxicity and changes in cytosolic calcium and mitochondrial membrane potential in human colon adenocarcinoma cell lines.
Berezesky, IK; Boder, GB; Jain, PT; Phelps, PC; Trump, BF, 1995
)
3.18

Toxicity

ExcerptReferenceRelevance
" Both drugs were more toxic to the tumorigenic cells than to the normal cells, but LY295501 was significantly more toxic to both cells."( Studies on the mechanism of sulofenur and LY295501 toxicity: effect on the regulation of cytosolic calcium in relation to cytotoxicity in normal and tumorigenic rat kidney cell lines.
Berezesky, IK; Best, CJ; Boder, GB; Merriman, RL; Phelps, PC; Tanzer, LR; Trump, BF, 1995
)
0.59
" No nucleosomal ladders were detected in quiescent cells during exposure to toxic concentrations of drug (IC90), or after removal of ISCU and addition of serum to stimulate growth."( Proliferation-dependent and -independent cytotoxicity by antitumor diarylsulfonylureas. Indication of multiple mechanisms of drug action.
Germain, GS; Harwood, FC; Houghton, PJ; Sosinski, J; Thakar, JH, 1993
)
0.29

Pharmacokinetics

ExcerptReferenceRelevance
" In all species, sulofenur was well absorbed after an oral dose, but over a prolonged period, and sulofenur exhibited a fairly long half-life of elimination from plasma."( Pharmacokinetics of the anticancer agent sulofenur in mice, rats, monkeys, and dogs.
Bewley, JR; Cornpropst, D; Ehlhardt, WJ; Grindey, GB; Hamilton, C; Hamilton, M; Sullivan, HR; Wood, PG; Woodland, JM; Worzalla, JF, 1993
)
0.89

Bioavailability

Sulofenur (I) is well absorbed in both monkey and human. practically all of the excreted radiolabel from an oral dose is in the urine.

ExcerptReferenceRelevance
" Further studies that attempt to increase the bioavailability and improve the therapeutic index are warranted."( A phase II study of sulofenur, a novel sulfonylurea, in recurrent epithelial ovarian cancer.
Hardy, J; Hatty, S; O'Brien, ME; Peters, B; Tan, S; Walling, J; Wiltshaw, E, 1992
)
0.61
" Sulofenur (I) is well absorbed in both monkey and human; practically all of the excreted radiolabel from an oral dose is in the urine."( Metabolism and disposition of the anticancer agent sulofenur in mouse, rat, monkey, and human.
Ehlhardt, WJ,
)
1.29
" In all species, sulofenur was well absorbed after an oral dose, but over a prolonged period, and sulofenur exhibited a fairly long half-life of elimination from plasma."( Pharmacokinetics of the anticancer agent sulofenur in mice, rats, monkeys, and dogs.
Bewley, JR; Cornpropst, D; Ehlhardt, WJ; Grindey, GB; Hamilton, C; Hamilton, M; Sullivan, HR; Wood, PG; Woodland, JM; Worzalla, JF, 1993
)
0.89

Dosage Studied

ExcerptRelevanceReference
" A maximum tolerated daily dosage was not defined, as methemoglobinemia was noted with each dosage level."( A phase I study of sulofenur in refractory pediatric malignant solid tumors.
Avery, L; Bowman, LC; Luo, X; Marina, N; Meyer, WH; Pappo, A; Pratt, CB, 1995
)
0.62
" In conclusion although sulofenur had only minor side effects, in the dosage and schedule used, it did not produce any significant response in advanced non-small cell lung cancer."( Phase II study of sulofenur (LY 186641). A novel antineoplastic agent in advanced non-small cell lung cancer.
Einhorn, LH; Fossella, F; Lippman, SM; Munshi, NC; Seitz, DE, 1993
)
0.93
" The dosage chosen on the basis of pre-clinical and phase I studies was 700 mg/m2 given orally once daily for 14 days, with treatments being repeated every 3 weeks."( Phase II trial of the novel sulphonylurea sulofenur in advanced breast cancer.
Button, D; Nicolson, MC; Powles, TJ; Smith, IE; Talbot, DC; Walling, J, 1993
)
0.55
" In general, several analogs demonstrated excellent growth inhibitory activity in the 6C3HED model when dosed orally or intraperitoneally."( Sulfonimidamide analogs of oncolytic sulfonylureas.
Bewley, JR; Boder, GB; Ehlhardt, WJ; Gates, SB; Grindey, GB; Klingerman, KK; Ray, JE; Rinzel, SM; Schultz, RM; Toth, JE; Weir, LC; Worzalla, JF, 1997
)
0.3
" The initial dosage was 250 mg/m2 escalating to 700 mg/m2 daily with no dose modification for the individual patient at any given dose level; 38 patients with advanced solid malignant tumours were enrolled."( Early clinical investigation of sulofenur with a daily schedule in advanced solid tumours.
Andersen, E; Andersen, H; Hansen, HH; Krarup-Hansen, A; Pedersen, H, 1997
)
0.58
" Both types of assayed compounds, the N-(2-pyridylsulfonyl)urea and N-(2-pyridylsulfenyl)urea derivatives, inhibited by 50% the growth of the CCRF-CEM cell line at a dosage near to 1 microM."( Synthesis and cytotoxic activity of N-(2-pyridylsulfenyl)urea derivatives. A new class of potential antineoplastic agents.
Arteaga, C; Encío, I; Gil, MJ; González, A; Mañú, MA; Martínez-Merino, V; Migliaccio, M, 1999
)
0.3
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (46)

Assay IDTitleYearJournalArticle
AID103635Antitumor activity in vivo expressed as percent of inhibition in Lewis-lung carcinoma cell line1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID117211In vivo antitumor activity against subaxillary implanted 6C3HED lymphosarcoma implanted in C3H mice at a dose of 150 mg/kg administered perorally twice daily for a period of 8 days.1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Sulfonimidamide analogs of oncolytic sulfonylureas.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID43977Antitumor activity in vivo expressed as percent of inhibition in C3H-mammary adenocarcinoma cell line; 95-100% inhibition1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID8666Cytotoxicity against human lung carcinoma A549 cell line using MTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and antitumor activity of 4-phenyl-1-arylsulfonyl imidazolidinones.
AID38317Antitumor activity in vivo expressed as percent of inhibition in B-16-melanoma (solid) cell line1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID111010Metabolic breakdown to the o-sulfate of p-chloroaniline (2-amino-5-chlorophenyl sulfate) by giving 100 mg/kg oral doses of the compound1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Sulfonimidamide analogs of oncolytic sulfonylureas.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID153377Antitumor activity in vivo and the activity was determined as percent increase in life span determined against P388-lymphocytic leukemia tumor cell lines; 50-99 %1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID94802Cytotoxicity against human chronic myelogenous leukemia (K562) cell line using MTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and antitumor activity of 4-phenyl-1-arylsulfonyl imidazolidinones.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID608341Anticancer activity against human KATO III cells by MTT assay2011European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
Structure--activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity.
AID608340Anticancer activity against human COLO205 cells by MTT assay2011European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
Structure--activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity.
AID106647Antitumor activity in vivo expressed as percent of inhibition in Madison-lung carcinoma cell line; 80-94% inhibition1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID608344Anticancer activity against mouse P388D1 cells by MTT assay2011European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
Structure--activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID43703Cytotoxicity against CCRF-CEM lymphocytic leukemia cell line1999Bioorganic & medicinal chemistry letters, Aug-16, Volume: 9, Issue:16
Synthesis and cytotoxic activity of N-(2-pyridylsulfenyl)urea derivatives. A new class of potential antineoplastic agents.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID42420Antitumor activity in vivo expressed as percent of inhibition in CA-755-mammary adenocarcinoma tumor cell line; 95-100% inhibition1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID189673Hypoglycemic activity expressed as (Maximum reduction in blood glucose in mg/dL relative to predosing glucose level)/(time in hours at which maximum reduction occurred)1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID7270Antitumor activity in vivo against the 6C3HED lymphosarcoma, dosed for 10 days at 300 mg/kg1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID202502Cytotoxicity against human ovarian adenocarcinoma (SK-OV-3) cell line using MTT assay1998Bioorganic & medicinal chemistry letters, Jun-16, Volume: 8, Issue:12
Synthesis and antitumor activity of 4-phenyl-1-arylsulfonyl imidazolidinones.
AID7290Antitumor activity in vivo expressed as percent of inhibition in 6C3HED-lymphosarcoma tumor cell line; 95-100% inhibition1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID103159Antitumor activity in vivo expressed as percent of inhibition in M-5-ovarian carcinoma cell line; 95-100% inhibition1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID44602Antitumor activity in vivo expressed as percent of inhibition in C-26-colon carcinoma cell line; 95-100% inhibition1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID608339Anticancer activity against human A549 cells by MTT assay2011European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
Structure--activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID219580Antitumor activity in vivo expressed as percent of inhibition in X5563-plasma cell myeloma cell line; 60-79 % inhibition1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID25331Affinity constant was determined along with the o-sulfate of p-chloroaniline (2-amino-5-chlorophenyl sulfate)1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Sulfonimidamide analogs of oncolytic sulfonylureas.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID608343Anticancer activity against human SKOV3 cells by MTT assay2011European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
Structure--activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID44016Concentration required to inhibit growth of CCRF-CEM cells in culture for 72 hr to 50% of control growth1990Journal of medicinal chemistry, Sep, Volume: 33, Issue:9
Novel agents effective against solid tumors: the diarylsulfonylureas. Synthesis, activities, and analysis of quantitative structure-activity relationships.
AID43708In vitro cytotoxicity against CCRF-CEM cells1997Journal of medicinal chemistry, Mar-14, Volume: 40, Issue:6
Sulfonimidamide analogs of oncolytic sulfonylureas.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID608342Anticancer activity against human K562 cells by MTT assay2011European journal of medicinal chemistry, Aug, Volume: 46, Issue:8
Structure--activity relationship studies of novel arylsulfonylimidazolidinones for their anticancer activity.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (51)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (9.80)18.7374
1990's36 (70.59)18.2507
2000's2 (3.92)29.6817
2010's2 (3.92)24.3611
2020's6 (11.76)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.36

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index16.36 (24.57)
Research Supply Index4.30 (2.92)
Research Growth Index5.49 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.36)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (25.86%)5.53%
Reviews3 (5.17%)6.00%
Case Studies1 (1.72%)4.05%
Observational0 (0.00%)0.25%
Other39 (67.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]