Page last updated: 2024-11-10

uc-781

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

Cross-References

ID SourceID
PubMed CID3000926
CHEMBL ID54893
SCHEMBL ID2670342
MeSH IDM0264149

Synonyms (38)

Synonym
NCI60_026594
nsc-675186
gna & uc-781
n-[4-chloro-3-(3-methyl-2-butenyloxy)phenyl]-2-methyl-3-furancarbothioamide & galanthus nivalis agglutinin (gna)
hha & uc-781
n-[4-chloro-3-(3-methyl-2-butenyloxy)phenyl]-2-methyl-3-furancarbothioamide & hippeastrum hybrid agglutinin( hha)
n-[4-chloro-3-(3-methylbut-2-enoxy)phenyl]-2-methyl-furan-3-carbothioamide
furancarbothioanilide deriv
178870-32-1
uc781
uc-781 ,
nsc675186
thiocarboxanilide
uc 781
n-[4-chloro-3-(3-methyl-2-butenyloxy)phenyl]-2-methyl-3-furancarbothioamide
2-methyl-furan-3-carbothioic acid [4-chloro-3-(3-methyl-but-2-enyloxy)-phenyl]-amide
UC1 ,
CHEMBL54893 ,
bdbm50105629
n-{4-chloro-3-[(3-methylbut-2-enyl)oxy]phenyl}-2-methylfuran-3-carbothioamide
n-(4-chloro-3-(3-methylbut-2-enyloxy)phenyl)-2-methylfuran-3-carbothioamide
n-[4-chloro-3-(3-methylbut-2-enoxy)phenyl]-2-methylfuran-3-carbothioamide
3-furancarbothioamide, n-(4-chloro-3-((3-methyl-2-butenyl)oxy)phenyl)-2-methyl-
n-(4-chloro-3-((3-methyl-2-butenyl)oxy)phenyl)-2-methyl-3-furancarbothioamide
nsc 675186
l7k247h29h ,
unii-l7k247h29h
3-furancarbothioamide, n-(4-chloro-3-((3-methyl-2-buten-1-yl)oxy)phenyl)-2-methyl-
DB05871
YZHIXLCGPOTQNB-UHFFFAOYSA-N
SCHEMBL2670342
DTXSID10170581
AKOS030541468
n-{4-chloro-3-[(3-methylbut-2-en-1-yl)oxy]phenyl}-2-methylfuran-3-carbothioamide
Q27096436
n-(4-chloro-3-((3-methylbut-2-en-1-yl)oxy)phenyl)-2-methylfuran-3-carbothioamide
A857056
3-furancarbothioamide, n-[4-chloro-3-[(3-methyl-2-buten-1-yl)oxy]phenyl]-2-methyl-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Both formulations were safe to the vaginal microenvironment, even with repeated daily use, as evidenced by colposcopy, cytokine analysis, and lack of impact on vaginal microflora."( Preclinical safety assessments of UC781 anti-human immunodeficiency virus topical microbicide formulations.
Balkus, JE; Hillier, SL; Moncla, BJ; Parniak, MA; Patton, DL; Rohan, LC; Sweeney, YT, 2007
)
0.34
" The most frequently reported adverse events were genitourinary; however, the placebo and UC781 arms had a similar distribution of mild and moderate genitourinary events."( The safety, persistence, and acceptability of an antiretroviral microbicide candidate UC781.
Bunge, K; Hillier, S; Macio, I; Meyn, L; Moncla, B; Noguchi, L; Parniak, MA; Schwartz, JL, 2012
)
0.38

Pharmacokinetics

ExcerptReferenceRelevance
" UC781 possesses a favorable pharmacokinetic profile in mice with a high level of oral bioavailability."( Efficacy, pharmacokinetics, and in vivo antiviral activity of UC781, a highly potent, orally bioavailable nonnucleoside reverse transcriptase inhibitor of HIV type 1.
Bader, JP; Bonomi, C; Borgel, S; Buckheit, RW; Decker, W; Elder, C; Fliakas-Boltz, V; Hollingshead, M; Malspeis, L; Pallansch, LA; Roberson, J; Shores, R; Siford, T; Stinson, S, 1997
)
0.3

Bioavailability

ExcerptReferenceRelevance
" Self-microemulsifying drug delivery systems (SMEDDSs) have been developed to enhance the water solubility and bioavailability of hydrophobic drugs, such as UC781."( Development and characterisation of a self-microemulsifying drug delivery systems (SMEDDSs) for the vaginal administration of the antiretroviral UC-781.
Friend, D; McConville, C, 2013
)
0.59

Dosage Studied

ExcerptRelevanceReference
" When evaluated in a murine hollow fiber implant model of HIV infection, UC781 dosed orally or parenterally was able to suppress HIV replication completely in this model system, providing evidence of the in vivo efficacy of the compound."( Efficacy, pharmacokinetics, and in vivo antiviral activity of UC781, a highly potent, orally bioavailable nonnucleoside reverse transcriptase inhibitor of HIV type 1.
Bader, JP; Bonomi, C; Borgel, S; Buckheit, RW; Decker, W; Elder, C; Fliakas-Boltz, V; Hollingshead, M; Malspeis, L; Pallansch, LA; Roberson, J; Shores, R; Siford, T; Stinson, S, 1997
)
0.3
" Five safety/pharmacokinetic studies of UC781 are currently underway in women and men, all utilizing UC781 concentrations less than 1%, with twice-daily dosing in some studies, and all involving careful monitoring of exposed epithelium."( A randomized six-day safety study of an antiretroviral microbicide candidate UC781, a non-nucleoside reverse transcriptase inhibitor.
Ballagh, SA; Callahan, MM; Douville, K; Kovalevsky, G; Lai, JJ; Mauck, CK; McCormick, T; Schwartz, JL, 2008
)
0.35
" The enhancement of UC781 aqueous solubility is essential for the development of a useful vaginal microbicide dosage form, and our data suggest that UC781/cyclodextrin inclusion complexes may be useful in this context."( Characterization of cyclodextrin inclusion complexes of the anti-HIV non-nucleoside reverse transcriptase inhibitor UC781.
Hillier, SL; Isaacs, CE; Parniak, MA; Rohan, LC; Yang, H, 2008
)
0.35
" Baseline, single-dose exposure and a separate, 7-day at-home dosing were assessed."( First phase 1 double-blind, placebo-controlled, randomized rectal microbicide trial using UC781 gel with a novel index of ex vivo efficacy.
Adler, A; Anton, PA; Boscardin, J; Carballo-DiƩguez, A; Cortina, G; Cumberland, WG; Dennis, R; Elliott, J; Gabelnick, H; Khanukhova, E; Mauck, C; McCormick, T; McGowan, I; Rabe, L; Saunders, T; Tanner, K; Ventuneac, A; Zhou, Y, 2011
)
0.37
" Precision analysis, linear and logistical correlational methods were applied to model the dose-response relationship."( Dose-response relationship between tissue concentrations of UC781 and explant infectibility with HIV type 1 in the RMP-01 rectal safety study.
Anton, P; Mauck, C; McGowan, I; Richardson-Harman, N, 2012
)
0.38
"The Microbicide Trials Network 003 study, a large phase IIb trial, was unable to show that daily dosing with 1% tenofovir vaginal gel was effective for HIV prevention."( Current status of topical antiretroviral chemoprophylaxis.
Szpir, M; Van Damme, L, 2012
)
0.38
" Phase II and III trials continue to explore different dosing strategies for topical products that contain one or more ARV agents."( Current status of topical antiretroviral chemoprophylaxis.
Szpir, M; Van Damme, L, 2012
)
0.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1EC50 (µMol)0.01650.00040.61539.7000AID199991; AID199996
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1Activity0.00900.00091.30738.0000AID199980
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (41)

Assay IDTitleYearJournalArticle
AID581811Antiviral activity against X4 tropic HIV1 3B infected in human TZM-b1 cells after 2 hrs by luciferase assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID323901Inhibition of HIV1 BaL binding to human Caco-2 cells relative to control2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effect of topical microbicides on infectious human immunodeficiency virus type 1 binding to epithelial cells.
AID323899Inhibition of HIV1 BaL binding to human A431 cells relative to control2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effect of topical microbicides on infectious human immunodeficiency virus type 1 binding to epithelial cells.
AID581814Antiviral activity against X4 tropic HIV1 NL4.3 infected in human TZM-b1 cells after 2 hrs by luciferase assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID259754Antiviral activity against wild-type HIV1 in MT2 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID581812Antiviral activity against R5 tropic HIV1 BaL infected in human TZM-b1 cells after 2 hrs by luciferase assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID581816Antiviral activity against X4 tropic HIV1 RF infected in human PBMC assessed as inhibition of p24 antigen production after 2 hrs by ELISA2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID1163230Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei brucei Squib427 assessed as reduction in parasite growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID581823Cytotoxicity against human PBMC by MTT assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID1163253Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID260237Antiviral activity against HIV1 3B in MT2 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID323902Inhibition of HIV1 LAI binding to human Caco-2 cells relative to control2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effect of topical microbicides on infectious human immunodeficiency virus type 1 binding to epithelial cells.
AID581820Antiviral activity against R5 tropic HIV1 YU.2 infected in human PBMC assessed as inhibition of p24 antigen production after 2 hrs by ELISA2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID323900Inhibition of HIV1 LAI binding to human A431 cells relative to control2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effect of topical microbicides on infectious human immunodeficiency virus type 1 binding to epithelial cells.
AID767492Intrinsic solubility of the compound in water at 25 degC after 7 days by HPLC analysis2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
AID1163232Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID226235Fold resistance (L100I/ WT) was determined2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID198070Inhibitory activity against E138K mutant reverse transcriptase2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
AID1163233Antiviral activity against HIV1 infected in human TZM-bl cells assessed as viral inhibition pre-incubated for 30 mins prior to infection measured after 48 hrs by2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID248354Concentration required to inhibit 50% viral production of human immunodeficiency virus type 1 (HIV-1-IIIB)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Hierarchical database screenings for HIV-1 reverse transcriptase using a pharmacophore model, rigid docking, solvation docking, and MM-PB/SA.
AID581813Antiviral activity against R5 tropic HIV1 YU.2 infected in human TZM-b1 cells after 2 hrs by luciferase assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID581810Antiviral activity against X4 tropic HIV1 RF infected in human TZM-b1 cells after 2 hrs by luciferase assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID1163234Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID323898Antiviral activity against HIV1 BaL assessed as logReduction in viral transmission from human A431 cells to human PBMC by ELISA2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Effect of topical microbicides on infectious human immunodeficiency virus type 1 binding to epithelial cells.
AID581817Cytotoxicity against human TZM-bl cells by MTT assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID1163255Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human O positive erythrocyte assessed as reduction in parasitemia after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID199996Effective concentration required against wild type HIV-1 reverse transcriptase2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID581822Antiviral activity against R5 tropic HIV1 R8.BaL infected in human PBMC assessed as inhibition of p24 antigen production after 2 hrs by ELISA2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID198230Inhibitory activity against wild-type HIV-1 reverse transcriptase2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
AID259755Cytotoxicity against MT2 cells2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Computer-aided design of non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID581815Antiviral activity against R5 tropic HIV1 R8.BaL infected in human TZM-b1 cells after 2 hrs by luciferase assay2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID450502Antiviral activity against Human immunodeficiency virus 1 3B2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
The search for potent, small molecule NNRTIs: A review.
AID581821Antiviral activity against X4 tropic HIV1 NL4.3 infected in human PBMC assessed as inhibition of p24 antigen production after 2 hrs by ELISA2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID1163231Antitrypanocidal activity against suramin-sensitive Trypanosoma brucei rhodesiense STIB-900 assessed as reduction in parasite growth after 72 hrs2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID1163254Antileishmanial activity against Leishmania infantum MHOM/MA (BE)/67 infected in primary peritoneal mouse macrophages assessed as reduction in parasite burdun2014Bioorganic & medicinal chemistry, Oct-01, Volume: 22, Issue:19
From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
AID199991Effective concentration required against L100I mutant HIV-1 reverse transcriptase2001Bioorganic & medicinal chemistry letters, Nov-05, Volume: 11, Issue:21
Antiviral drug design: computational analyses of the effects of the L100I mutation for HIV-RT on the binding of NNRTIs.
AID260238Cytotoxicity against human MT2 cells by MTT assay2006Bioorganic & medicinal chemistry letters, Feb, Volume: 16, Issue:3
Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
AID302621Cytotoxicity against human MT2 cells by MTT assay2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
From docking false-positive to active anti-HIV agent.
AID199980Inhibitory activity against human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT)2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
Prediction of activity for nonnucleoside inhibitors with HIV-1 reverse transcriptase based on Monte Carlo simulations.
AID581819Antiviral activity against HIV1 A17 harboring reverse transcriptase K103N, Y181C mutant infected in human TZM-b1 cells after 2 hrs by luciferase assays2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Reverse transcriptase inhibitors as potential colorectal microbicides.
AID198106Inhibitory activity against R172A mutant reverse transcriptase2001Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (70)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's10 (14.29)18.2507
2000's35 (50.00)29.6817
2010's25 (35.71)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: 10.31

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 Index10.31 (24.57)
Research Supply Index4.34 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (8.57%)5.53%
Reviews3 (4.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other61 (87.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (5)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase I Trial of the Safety, Toxicity, and Acceptability of the Microbicide UC-781 When Topically Applied by HIV-uninfected Women and Men in Botswana [NCT00385554]Phase 10 participants (Actual)InterventionalWithdrawn(stopped due to Study product is no longer being considered for further development.)
A Phase 1 Randomized, Blinded, Placebo-Controlled Safety and Acceptability Study of the UC-781 Vaginal Microbicide Gel Formulation Applied Rectally in HIV-1 Seronegative Adults [NCT00408538]Phase 136 participants (Anticipated)Interventional2006-12-31Completed
Phase I Study of the Safety and Acceptability of UC-781 Topical Vaginal Microbicide in Women and Acceptability in Their Male Partners,Chiang Rai, Thailand [NCT00446979]Phase 190 participants (Actual)Interventional2007-06-30Completed
Phase I Study of the Safety and Persistence of 0.1% UC-781 Vaginal Gel in HIV-1 Seronegative Women [NCT00441909]Phase 160 participants (Anticipated)Interventional2006-04-30Completed
Phase I Study of the Safety and Acceptability of UC-781 Topical Vaginal Microbicide in Heterosexual Women and Their Male Partners [NCT00132444]Phase 190 participants (Anticipated)Interventional2005-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]