pyridostatin profile

pyridostatin: binds telomeric G-quadruplexes; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	25227847
CHEMBL ID	2349416
SCHEMBL ID	24711398
MeSH ID	M0568264

Synonym
1085412-37-8
4-(2-aminoethoxy)-n2,n6-bis(4-(2-aminoethoxy)quinolin-2-yl)pyridine-2,6-dicarboxamide
pyridostatin
CHEMBL2349416
CS-1439
HY-15176
rr-82
AKOS026750251
EX-A869
pyridostain
4-(2-aminoethoxy)-n2,n6-bis[4-(2-aminoethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide
NCGC00357427-06
BCP07688
rr 82
AS-16720
4-(2-aminoethoxy)-2-n,6-n-bis[4-(2-aminoethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide
NCGC00357427-11
4-(2-azanylethoxy)-n2,n6-bis[4-(2-azanylethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide
SCHEMBL24711398
4-(2-aminoethoxy)-n2,n6-bis[4-(2-aminoethoxy)-2-quinolinyl]-2,6-pyridinedicarboxamide, trifluoroacetate salt
AC-36193

Excerpt	Reference	Relevance
"Pyridostatin is a small molecule that binds G4s and is specifically toxic to BRCA1/2-deficient cells in vitro."	( Anti-tumoural activity of the G-quadruplex ligand pyridostatin against BRCA1/2-deficient tumours. Benainous, H; Biroccio, A; Bruna, A; De Visser, Y; Di Vito, S; Groelly, FJ; Kosova, AA; Leonetti, C; Porru, M; Ryan, A; Serra, V; Tarsounas, M; Zimmer, J, 2022)	1.7
"Pyridostatin (PDS) is a well-known G-quadruplex (G4) inducer and stabilizer, yet its target genes have remained unclear. "	( G-quadruplex inducer/stabilizer pyridostatin targets SUB1 to promote cytotoxicity of a transplatinum complex. Fang, T; Gan, T; Han, J; Hou, Y; Jia, F; Li, S; Liu, X; Luo, Q; Qi, L; Wang, F; Wang, S; Zhang, Y; Zhao, Y, 2022)	2.45

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Bioassays (22)

Assay ID	Title	Year	Journal	Article
AID1473368	Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for bloodstream form of Trypanosoma brucei brucei	2018	Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3	G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID1290618	Ratio of binding affinity to Bcl2 G-quadruplex DNA (unknown origin) to binding affinity to duplex ds26 DNA (unknown origin)	2016	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7	Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog.
AID1473363	Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei after 72 hrs by alamar blue assay	2018	Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3	G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID1875179	Cytotoxicity against mouse MNMCA1 cells assessed as cell survival preincubated for 24 hrs with compound further incubated for 48 hrs in drug free medium by MTT assay	2022	Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18	Balancing Affinity, Selectivity, and Cytotoxicity of Hydrazone-Based G-Quadruplex Ligands for Activation of Interferon β Genes in Cancer Cells.
AID1290613	Binding affinity to duplex ds20 DNA (unknown origin) assessed as binding constant at 8 uM by Stern-Volmer plot analysis in the presence of KCl and NaCl	2016	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7	Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog.
AID1473364	Antileishmanial activity against Leishmania major MHOM/IL/80/Friedlin promastigotes after 72 hrs by MTT assay	2018	Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3	G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID1473365	Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 72 hrs by MTT assay	2018	Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3	G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID1290614	Binding affinity to duplex ds26 DNA (unknown origin) assessed as binding constant at 8 uM by Stern-Volmer plot analysis in the presence of KCl and NaCl	2016	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7	Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog.
AID1473369	Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for erythrocyte stage of Plasmodium falciparum 3D7	2018	Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3	G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID1473366	Antimalarial activity against erythrocyte stage of Plasmodium falciparum 3D7 preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting	2018	Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3	G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID1473367	Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for Leishmania major MHOM/IL/80/Friedlin promastigotes	2018	Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3	G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents.
AID737820	Thermal stabilization of human telomeric G-quadruplex FAM-TTAGGGTTAGGGTTAGGGTTAGGG-TAMRA DNA assessed as change in melting temperature at 1:5 DNA:ligand ratio by FRET assay	2013	Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7	Guanidino anthrathiophenediones as G-quadruplex binders: uptake, intracellular localization, and anti-Harvey-Ras gene activity in bladder cancer cells.
AID1290622	Ratio of binding affinity to Bcl2 G-quadruplex DNA (unknown origin) to binding affinity to duplex ds20 DNA (unknown origin)	2016	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7	Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog.
AID1290612	Binding affinity to Bcl2 G-quadraplex DNA (unknown origin) assessed as binding constant at 8 uM by Stern-Volmer plot analysis in the presence of KCl and NaCl	2016	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7	Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog.
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1794808	Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).	2014	Journal of biomolecular screening, Jul, Volume: 19, Issue:6	A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808	Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	35 (57.38)	24.3611
2020's	26 (42.62)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	2 (3.28%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	59 (96.72%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
berberine [no description available]	2.21	1	alkaloid antibiotic; berberine alkaloid; botanical anti-fungal agent; organic heteropentacyclic compound	antilipemic drug; antineoplastic agent; antioxidant; EC 1.1.1.141 [15-hydroxyprostaglandin dehydrogenase (NAD(+))] inhibitor; EC 1.1.1.21 (aldehyde reductase) inhibitor; EC 1.13.11.52 (indoleamine 2,3-dioxygenase) inhibitor; EC 1.21.3.3 (reticuline oxidase) inhibitor; EC 2.1.1.116 [3'-hydroxy-N-methyl-(S)-coclaurine 4'-O-methyltransferase] inhibitor; EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor; EC 2.7.11.10 (IkappaB kinase) inhibitor; EC 3.1.1.4 (phospholipase A2) inhibitor; EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor; EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; geroprotector; hypoglycemic agent; metabolite; potassium channel blocker
chlorambucil Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.	2.1	1	aromatic amine; monocarboxylic acid; nitrogen mustard; organochlorine compound; tertiary amino compound	alkylating agent; antineoplastic agent; carcinogenic agent; drug allergen; immunosuppressive agent
chloroquine Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.	2.17	1	aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug
miltefosine miltefosine: hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin. miltefosine : A phospholipid that is the hexadecyl monoester of phosphocholine.	2.17	1	phosphocholines; phospholipid	anti-inflammatory agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antiprotozoal drug; apoptosis inducer; immunomodulator; protein kinase inhibitor
mitoxantrone Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.	2.21	1	dihydroxyanthraquinone	analgesic; antineoplastic agent
potassium chloride Potassium Chloride: A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.. potassium chloride : A metal chloride salt with a K(+) counterion.	2.17	1	inorganic chloride; inorganic potassium salt; potassium salt	fertilizer
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.	2.21	1	mitomycin	alkylating agent; antineoplastic agent
tromethamine Tromethamine: An organic amine proton acceptor. It is used in the synthesis of surface-active agents and pharmaceuticals; as an emulsifying agent for cosmetic creams and lotions, mineral oil and paraffin wax emulsions, as a biological buffer, and used as an alkalizer. (From Merck, 11th ed; Martindale, The Extra Pharmacopoeia, 30th ed, p1424)	2.25	1	primary amino compound; triol	buffer
acridines Acridines: Compounds that include the structure of acridine.. acridine : A polycyclic heteroarene that is anthracene in which one of the central CH groups is replaced by a nitrogen atom.	3.13	4	acridines; mancude organic heterotricyclic parent; polycyclic heteroarene	genotoxin
oxazoles Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.	2.52	2	1,3-oxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
braco-19 BRACO-19: structure in first source	3.31	5	acridines; N-alkylpyrrolidine
nu 7441 8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one: structure in first source	2.08	1	dibenzothiophenes
telomestatin telomestatin: isolated from Spreptomyces anulatus; structure in first source	2.52	2
oligonucleotides [no description available]	2.58	2
cx 5461 CX 5461: structure in first source	2.72	2	diazepine; naphthyridine derivative; organic heterotetracyclic compound; pyrazines; secondary carboxamide	antineoplastic agent; apoptosis inducer; EC 2.7.7.6 (RNA polymerase) inhibitor
tetra(4-n-methylpyridyl)porphine tetra(4-N-methylpyridyl)porphine: structure in first source	2.21	1
guanine [no description available]	3.35	1	2-aminopurines; oxopurine; purine nucleobase	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
guanosine ribonucleoside : Any nucleoside where the sugar component is D-ribose.	2.15	1	guanosines; purines D-ribonucleoside	fundamental metabolite

Condition	Relationship Strength	Studies
Bladder Cancer [description not available]	2.08	1
Urinary Bladder Neoplasms Tumors or cancer of the URINARY BLADDER.	2.08	1
Plasmodium falciparum Malaria [description not available]	2.1	1
Malaria, Falciparum Malaria caused by PLASMODIUM FALCIPARUM. This is the severest form of malaria and is associated with the highest levels of parasites in the blood. This disease is characterized by irregularly recurring febrile paroxysms that in extreme cases occur with acute cerebral, renal, or gastrointestinal manifestations.	2.1	1
Carcinoma, Epidermoid [description not available]	2.13	1
Cancer of Larynx [description not available]	2.13	1
Carcinoma, Squamous Cell A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)	2.13	1
Laryngeal Neoplasms Cancers or tumors of the LARYNX or any of its parts: the GLOTTIS; EPIGLOTTIS; LARYNGEAL CARTILAGES; LARYNGEAL MUSCLES; and VOCAL CORDS.	2.13	1
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.25	1
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1
Genome Instability [description not available]	3.88	3
Benign Neoplasms [description not available]	3.45	6
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	3.45	6
Enterovirus Infections Diseases caused by ENTEROVIRUS.	3.23	1
Hepatitis B Virus Infection [description not available]	2.6	1
Hepatitis B INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.	2.6	1
Breast Cancer [description not available]	2.85	3
Breast Neoplasms Tumors or cancer of the human BREAST.	2.85	3
Age-Related Memory Disorders [description not available]	2.25	1
Memory Disorders Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.	2.25	1
Infections, Plasmodium [description not available]	2.25	1
Malaria A protozoan disease caused in humans by four species of the PLASMODIUM genus: PLASMODIUM FALCIPARUM; PLASMODIUM VIVAX; PLASMODIUM OVALE; and PLASMODIUM MALARIAE; and transmitted by the bite of an infected female mosquito of the genus ANOPHELES. Malaria is endemic in parts of Asia, Africa, Central and South America, Oceania, and certain Caribbean islands. It is characterized by extreme exhaustion associated with paroxysms of high FEVER; SWEATING; shaking CHILLS; and ANEMIA. Malaria in ANIMALS is caused by other species of plasmodia.	2.25	1
Catarrh Inflammation of a mucous membrane with increased flow of mucous in humans or animals. Catarrh is used mostly in a historical context.	2.25	1
Common Cold A catarrhal disorder of the upper respiratory tract, which may be viral or a mixed infection. It generally involves a runny nose, nasal congestion, and sneezing.	7.25	1
Viral Diseases [description not available]	2.31	1
Virus Diseases A general term for diseases caused by viruses.	2.31	1
B16 Melanoma [description not available]	2.31	1
Chromosome-Defective Micronuclei [description not available]	2.31	1
Cell Transformation, Neoplastic Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.	2.17	1
Chromosomal Translocation [description not available]	2.17	1
Adenocarcinoma Of Kidney [description not available]	2.17	1
Cancer of Kidney [description not available]	2.17	1
Carcinoma, Renal Cell A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.	2.17	1
Kidney Neoplasms Tumors or cancers of the KIDNEY.	2.17	1
Epithelial Neoplasms [description not available]	2.08	1

pyridostatin

Description

Cross-References

Synonyms (21)

Research Excerpts

Overview

Bioavailability

Bioassays (22)

Research

Studies (61)

Market Indicators

Research Demand Index: 34.83

Study Types

pyridostatin

Description

Cross-References

Synonyms (21)

Research Excerpts

Overview

Bioavailability

Bioassays (22)

Research

Studies (61)

Market Indicators

Research Demand Index: 34.83

Study Types

Related Drugs (18)

Related Conditions (36)