Page last updated: 2024-12-07

uk 1

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

Description

UK 1: a cytotoxic metabolite from Streptomyces sp. 517-02; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	127748
CHEMBL ID	111574
SCHEMBL ID	11979724
MeSH ID	M0220477

Synonyms (19)

Synonym
methyl 2-(2-(2-hydroxyphenyl)benzo[d]oxazol-4-yl)benzo[d]oxazole-4-carboxylate
bdbm50147399
2''-(2-hydroxy-phenyl)-[2,4'']bibenzooxazolyl-4-carboxylic acid methyl ester
uk 1
CHEMBL111574 ,
151271-53-3
methyl 2'-(2-hydroxyphenyl)-(2,4'-bibenzoxazole)-4-carboxylate
uk-1
(2,4'-bibenzoxazole)-4-carboxylic acid, 2'-(2-hydroxyphenyl)-, methyl ester
methyl 2-[2-(2-hydroxyphenyl)-1,3-benzoxazol-4-yl]-1,3-benzoxazole-4-carboxylate
SCHEMBL11979724
HB4117
methyl 2'-(2-hydroxyphenyl)-oxazole]-4-carboxylate; 2'-(2-hydroxyphenyl)-(2,4'-bibenzoxazole)-4-carboxylic acid methyl ester
J-008796
methyl 2'-(2-hydroxyphenyl)-[2,4'-bibenzo[d]oxazole]-4-carboxylate
[2,4'-bibenzoxazole]-4-carboxylic acid, 2'-(2-hydroxyphenyl)-, methyl ester
2'-(2-hydroxyphenyl)-[2,4'-bibenzoxazole]-4-carboxylic acid, methyl ester
CS-0106677
HY-129558

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
DNA topoisomerase 2-alpha	Homo sapiens (human)	IC50 (µMol)	41.0000	0.4800	4.3564	9.9400	AID57356; AID57357
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Process	via Protein(s)	Taxonomy
hematopoietic progenitor cell differentiation	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA topological change	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA ligation	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA damage response	DNA topoisomerase 2-alpha	Homo sapiens (human)
chromosome segregation	DNA topoisomerase 2-alpha	Homo sapiens (human)
female meiotic nuclear division	DNA topoisomerase 2-alpha	Homo sapiens (human)
apoptotic chromosome condensation	DNA topoisomerase 2-alpha	Homo sapiens (human)
embryonic cleavage	DNA topoisomerase 2-alpha	Homo sapiens (human)
regulation of circadian rhythm	DNA topoisomerase 2-alpha	Homo sapiens (human)
positive regulation of apoptotic process	DNA topoisomerase 2-alpha	Homo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediate	DNA topoisomerase 2-alpha	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	DNA topoisomerase 2-alpha	Homo sapiens (human)
rhythmic process	DNA topoisomerase 2-alpha	Homo sapiens (human)
negative regulation of DNA duplex unwinding	DNA topoisomerase 2-alpha	Homo sapiens (human)
resolution of meiotic recombination intermediates	DNA topoisomerase 2-alpha	Homo sapiens (human)
sister chromatid segregation	DNA topoisomerase 2-alpha	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Process	via Protein(s)	Taxonomy
magnesium ion binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
chromatin binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
RNA binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activity	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein kinase C binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
ATP binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
ATP-dependent activity, acting on DNA	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA binding, bending	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein homodimerization activity	DNA topoisomerase 2-alpha	Homo sapiens (human)
ubiquitin binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein heterodimerization activity	DNA topoisomerase 2-alpha	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Process	via Protein(s)	Taxonomy
nucleolus	DNA topoisomerase 2-alpha	Homo sapiens (human)
nuclear chromosome	DNA topoisomerase 2-alpha	Homo sapiens (human)
centriole	DNA topoisomerase 2-alpha	Homo sapiens (human)
chromosome, centromeric region	DNA topoisomerase 2-alpha	Homo sapiens (human)
condensed chromosome	DNA topoisomerase 2-alpha	Homo sapiens (human)
male germ cell nucleus	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleus	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleoplasm	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleolus	DNA topoisomerase 2-alpha	Homo sapiens (human)
cytoplasm	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complex	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein-containing complex	DNA topoisomerase 2-alpha	Homo sapiens (human)
ribonucleoprotein complex	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleus	DNA topoisomerase 2-alpha	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (27)

Assay ID	Title	Year	Journal	Article
AID320493	Cytotoxicity against human MCF7 cells after 72 hrs in presence of CuCl2	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID373320	Cytotoxicity against human MCF7 cells after 72 hrs by Alamar Blue assay	2009	European journal of medicinal chemistry, Apr, Volume: 44, Issue:4	New transition metal ion complexes with benzimidazole-5-carboxylic acid hydrazides with antitumor activity.
AID718400	Cytotoxicity against human A549 cells after 72 hrs by alamar blue assay	2012	Bioorganic & medicinal chemistry, Dec-15, Volume: 20, Issue:24	Synthesis and docking studies of novel antitumor benzimidazoles.
AID150661	Inhibitory activity of compound against P388 murine cell line; range is 0.3 uM-1.6 uM	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
AID320488	Cytotoxicity against human A549 cells by Alamar blue assay	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID1063618	Inhibition of Dengue virus helicase	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID1063614	Antiviral activity against HCV infected in human Huh7ET cells assessed as inhibition of viral replication by luciferase reporter gene assay/RNA blot hybridization analysis	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID320495	Cytotoxicity against human A549 cells after 72 hrs	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID1063619	Inhibition of Japanese encephalitis virus helicase	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID320487	Cytotoxicity against human MCF7 cells by Alamar blue assay	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID1063612	Cytotoxicity against human Huh7ET cells by neutral red assay	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID156163	Cytotoxicity of compound against PC-3 cell line	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
AID82838	Cytotoxicity of compound against HL60 cell line	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
AID1063617	Inhibition of HCV NS3 NTPase/helicase domain expressed in Escherichia coli BL21 using dsDNA as substrate assessed as strand separation of [32P]-labeled oligonucleotides after 30 mins by SDS-gel electrophoresis	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID57357	Inhibitory concentration against human DNA topoisomerase II, alpha mediated relaxation of pBR322	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
AID320494	Cytotoxicity against human A549 cells after 24 hrs	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID57356	Inhibitory activity of compound against human DNA topoisomerase II, alpha was evaluated by ability to interfere with the relaxation of supercoiled plasmid DNA	2004	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12	Critical structural motif for the catalytic inhibition of human topoisomerase II by UK-1 and analogs.
AID1063615	Inhibition of HCV ATPase activity of NS3 NTPase/helicase domain expressed in Escherichia coli BL21 after 30 mins by thin layer chromatography in presence of [gamma-32P]ATP	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID320496	Cytotoxicity against human A549 cells after 24 hrs in presence of CuCl2	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID1063613	Inhibition of HCV NS5B RNA dependent RNA polymerase at 100 uM	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID1063610	Selectivity index, ratio of CC50 for human Huh7ET cells to EC50 for HCV infected in human Huh7ET cells	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID373321	Cytotoxicity against human A549 cells after 72 hrs by Alamar Blue assay	2009	European journal of medicinal chemistry, Apr, Volume: 44, Issue:4	New transition metal ion complexes with benzimidazole-5-carboxylic acid hydrazides with antitumor activity.
AID320497	Cytotoxicity against human A549 cells after 72 hrs in presence of CuCl2	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID1063616	Inhibition of HCV NS3 NTPase/helicase domain expressed in Escherichia coli BL21 using dsRNA as substrate assessed as strand separation of [32P]-labeled oligonucleotides after 30 mins by SDS-gel electrophoresis	2014	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 24, Issue:2	UK-1 and structural analogs are potent inhibitors of hepatitis C virus replication.
AID320492	Cytotoxicity against human MCF7 cells after 24 hrs in presence of CuCl2	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID320490	Cytotoxicity against human MCF7 cells after 24 hrs	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
AID320491	Cytotoxicity against human MCF7 cells after 72 hrs	2008	Bioorganic & medicinal chemistry, Feb-15, Volume: 16, Issue:4	Synthesis, metal ion binding, and biological evaluation of new anticancer 2-(2'-hydroxyphenyl)benzoxazole analogs of UK-1.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	3 (27.27)	18.2507
2000's	6 (54.55)	29.6817
2010's	2 (18.18)	24.3611
2020's	0 (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: 50.07

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 very strong demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	50.07 (24.57)
Research Supply Index	2.48 (2.92)
Research Growth Index	4.51 (4.65)
Search Engine Demand Index	72.96 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (50.07)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
adenine [no description available]	1.99	1	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
stallimycin [no description available]	2	1
mitomycin Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.. mitomycin : A family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae.	2.74	3	mitomycin	alkylating agent; antineoplastic agent
benzoxazoles 1,3-benzoxazole : A benzoxazole in which the benzene ring is fused to a 1,3-oxazole ring across positions 4 and 5.. benzoxazole : Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton.	3.62	9	1,3-benzoxazoles; mancude organic heterobicyclic parent
oleanolic acid [no description available]	2.07	1	hydroxy monocarboxylic acid; pentacyclic triterpenoid	plant metabolite
cefoperazone Cefoperazone: Semisynthetic broad-spectrum cephalosporin with a tetrazolyl moiety that is resistant to beta-lactamase. It may be used to treat Pseudomonas infections.. cefoperazone : A semi-synthetic parenteral cephalosporin with a tetrazolyl moiety that confers beta-lactamase resistance.	2.05	1	cephalosporin	antibacterial drug
tamoxifen [no description available]	2.07	1	stilbenoid; tertiary amino compound	angiogenesis inhibitor; antineoplastic agent; bone density conservation agent; EC 1.2.3.1 (aldehyde oxidase) inhibitor; EC 2.7.11.13 (protein kinase C) inhibitor; estrogen antagonist; estrogen receptor antagonist; estrogen receptor modulator
b 428 4-iodine-benzo(b)thiophene-2-carboxamidine: structure in first source	2.07	1
chromomycin a3 Chromomycin A3: Glycosidic antibiotic from Streptomyces griseus used as a fluorescent stain of DNA and as an antineoplastic agent.	2	1

Condition	Relationship Strength	Studies
Breast Cancer [description not available]	2.46	2
Cancer of Lung [description not available]	2.46	2
Breast Neoplasms Tumors or cancer of the human BREAST.	2.46	2
Lung Neoplasms Tumors or cancer of the LUNG.	2.46	2

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