Compounds > retelliptine
Page last updated: 2024-11-06

retelliptine

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Description

Retelliptine is a synthetic compound with a unique chemical structure, belonging to the family of ellipticine derivatives. It exhibits potent antitumor activity against various cancer cell lines, including those resistant to conventional chemotherapy. Research suggests that its mechanism of action involves intercalation with DNA, inhibiting DNA replication and transcription. Retelliptine has shown promising results in preclinical studies and is currently under investigation as a potential anticancer drug. Its unique structure and strong antitumor activity make it an attractive candidate for further development and clinical trials.'

retelliptine: structure given in first source; SR-95325 B (NSC-D626717) is the dihydrochloride [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID68913
CHEMBL ID279890
SCHEMBL ID61452
MeSH IDM0134353

Synonyms (33)

Synonym
nsc-d-626717-w
sr-95325a
retelliptine
bd-84
sr-95325b
peliptil
n,n-diethyl-n'-(9-methoxy-5,11-dimethyl-6h-pyrido(4,3-b)carbazol-1-yl)-1,3-propanediamine
retelliptine [inn]
brn 0718451
1-((3-(diethylamino)propyl)amino)-9-methoxy-5,11-dimethyl-6h-pyrido(4,3-b)carbazole
n,n-diethyl-n'-(9-methoxy-5,11-dimethyl-6h-pyrido(4,3-b)carbazol-1-yl)propane-1,3-diamine
6h-pyrido(4,3-b)carbazole, 1-((3-diethylamino)propylamino)-5,11-dimethyl-9-methoxy-
bd 84
retelliptinum [latin]
1,3-propanediamine, n,n-diethyl-n'-(9-methoxy-5,11-dimethyl-6h-pyrido(4,3-b)carbazol-1-yl)-
1-((3-(diethylamino)propyl)amino)-5,11-dimethyl-9-methoxy-6h-pyrido(4,3-b)carbazole
petelliptine [french]
reteliptina [spanish]
einecs 276-512-5
CHEMBL279890
n',n'-diethyl-n-(9-methoxy-5,11-dimethyl-6h-pyrido[4,3-b]carbazol-1-yl)propane-1,3-diamine
unii-sz0f94m68j
petelliptine
reteliptina
retelliptinum
sz0f94m68j ,
72238-02-9
SCHEMBL61452
AKOS022185032
DTXSID10222559
n1,n1-diethyl-n3-(9-methoxy-5,11-dimethyl-6h-pyrido[4,3-b]carbazol-1-yl)propane-1,3-diamine
sodiumsulfadiazine
Q27289475
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (40)

Assay IDTitleYearJournalArticle
AID137845Antitumor activity against P388 leukemia in mice at a dose of 24 mg/kg administered intraperitoneally for 5 days1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID96956Antitumor activity against L1210 leukemia cells measured as percent increase in life span (% ILS) at 10 mg/kg1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications.
AID137838Antitumor activity against P388 leukemia in mice at a dose of 16 mg/kg administered intraperitoneally for 5 days1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID225203Tested for medium tumor weight of treated /control animals x 100 (% T/C) for murine solid tumor model 3LL advanced stage that is subcutaneously implanted by the intravenous treatment at the dose of 2.5 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID225209Tested for medium tumor weight of treated /control animals x 100 (% T/C) for murine solid tumor model C26 early stage that is subcutaneously implanted by the intravenous treatment at the dose of 2.5 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID154582In vivo T/C (survival time treated/survival time control x 100) was determined against P388 leukemia cells at 10 mg/Kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID137697Antitumor activity against P388 leukemia in mice at a dose of 0.5 mg/kg administered intraperitoneally for 5 days1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID137859Antitumor activity against P388 leukemia in mice at a dose of 8 mg/kg administered intraperitoneally for 5 days1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID225208Tested for the change in body weight between day1 and 7 for murine solid tumor model B16 early stage that is subcutaneously implanted by the intravenous treatment at the dose of 1.25 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID115826In Vivo evaluation for the antitumor activity on grafted tumor friend cells at the dose 20 mg/kg and Increase in the life span was determined1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID225205Tested for the change in body weight between day1 and 7 for murine solid tumor model 3LL advanced stage that is subcutaneously implanted by the intravenous treatment at the dose of 2.5 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID116131In vivo evaluation for the antitumor activity on L1210 leukemia cells at the dose 15 mg/kg administered intraperitoneally estimated as increase in life span1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID54244B app constant towards DNA1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID97886Cytotoxicity against L1210 tumor cell line, activity is expressed as K (inverse value of drug concentration)1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications.
AID116587In Vivo antitumor activity on grafted tumor friend cells at the dose 20 mg/kg and decrease in intravenous 10 e 6 cells and median survival time1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID98677In vitro concentration required for growth inhibition of murine L1210 tumor cell1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID212886Acute toxicity in mice (LD0) after i.p. administration (highest nontoxic dose)1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications.
AID116712In vivo acute toxicity (lethal dose) against mice by intraperitoneal administration1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID119394In vivo antitumor activity on L1210 leukemia cells at the dose 15 mg/kg administered intraperitoneally estimated as range of deaths1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID98440Antitumor activity against L1210 leukemia cells measured as Median survival time at 15 mg/kg1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications.
AID98981Antitumor activity against L1210 leukemia cells measured as range of death at 15 mg/kg; value may range from 19 to 351983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications.
AID137851Antitumor activity against P388 leukemia in mice at a dose of 4 mg/kg administered intraperitoneally1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID137699Antitumor activity against P388 leukemia in mice at a dose of 1 mg/kg administered intraperitoneally for 5 days1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID212887Acute toxicity in mice (LD100) after i.p. administration1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications.
AID225207Tested for medium tumor weight of treated /control animals x 100 (% T/C) for murine solid tumor model B16 early stage that is subcutaneously implanted by the intravenous treatment at the dose of 1.25 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID116745In vivo evaluation for the antitumor activity on L1210 leukemia cells at the dose 15 mg/kg administered intraperitoneally estimated as Mean survival time1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID116697In vivo acute toxicity (nonlethal dose) against mice by intraperitoneal administration1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID225206Tested for the change in body weight between day1 and 7 for murine solid tumor model 3LL early stage that is subcutaneously implanted by the intravenous treatment at the dose of 2.5 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID225211Tested for the change in body weight between day1 and 7 for murine solid tumor model C26 early stage that is subcutaneously implanted by the intravenous treatment at the dose of 2.5 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID116713In vivo acute toxicity (lethal dose) against mice by intravenous administration1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID116699In vivo acute toxicity (nonlethal dose) against mice by intravenous administration1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID137839Antitumor activity against P388 leukemia in mice at a dose of 2 mg/kg administered intraperitoneally for 5 days1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID54613Apparent association constant towards DNA at concentration of 10e-7/M1980Journal of medicinal chemistry, Nov, Volume: 23, Issue:11
Structure-activity relationships in a series of newly synthesized 1-amino-substituted ellipticine derivatives.
AID225214Tested for the change in body weight between day1 and 7 for murine solid tumor model MA 16/C early stage that is subcutaneously implanted by the intravenous treatment at the dose of 2.5 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID224102In vivo total number of survivors was determined against L1210 Leukemia cells out of 8 mouse at 50 day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID225213Tested for medium tumor weight of treated /control animals x 100 (% T/C) for murine solid tumor model MA 16/C early stage that is subcutaneously implanted by the intravenous treatment at the dose of 2.5 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID54468Apparent DNA affinity constant1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID225204Tested for medium tumor weight of treated /control animals x 100 (% T/C) for murine solid tumor model 3LL early stage that is subcutaneously implanted by the intravenous treatment at the dose of 2.5 mg/kg in 1-4 schedule1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents.
AID96625Ability to reduce the cell count to 50% in L1210 culture cells1988Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
1-Amino-substituted 4-methyl-5H-pyrido[4,3-b]indoles (gamma-carbolines) as tricyclic analogues of ellipticines: a new class of antineoplastic agents.
AID96801In vitro cytotoxicity against L1210 cell line as concentration required for 50% inhibition of cell growth1983Journal of medicinal chemistry, Feb, Volume: 26, Issue:2
Antitumor amino-substituted pyrido[3',4':4,5]pyrrolo[2,3-g]isoquinolines and pyrido[4,3-b]carbazole derivatives: synthesis and evaluation of compounds resulting from new side chain and heterocycle modifications.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (37.50)18.7374
1990's5 (62.50)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: 12.17

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 Index12.17 (24.57)
Research Supply Index2.40 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.17)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (11.11%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
diaziquone
diaziquone: RN given refers to parent cpd. diaziquone : A 1,4-benzoquinone that is substituted at positions 2 and 5 have been replaced by aziridin-1-yl groups and at positions 3 and 6 by (ethoxycarbonyl)amino groups.		1.98101,4-benzoquinones;
aziridines;
carbamate ester;
enamine		alkylating agent;
antineoplastic agent
elliptinium
elliptinium: synthetic ellipticine deriv; RN given refers to parent cpd; structure given in first source		1.9510carbazoles
intoplicine
intoplicine: structure in first source		1.9710pyridoindole
pazelliptine
pazelliptine: RN given refers to parent cpd; structure given in first source		2.8940
9-methoxyellipticine
9-methoxyellipticine: RN given refers to parent cpd		1.9510
dactinomycin
Dactinomycin: A compound composed of a two CYCLIC PEPTIDES attached to a phenoxazine that is derived from STREPTOMYCES parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)		2.3620actinomycinmutagen
ConditionIndicatedRelationship StrengthStudiesTrials
Experimental Leukemia
[description not available]		01.9710
Experimental Neoplasms
[description not available]		02.3720
Leukemia L 1210
[description not available]		01.9610
Benign Neoplasms
[description not available]		03.3711
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.		03.3711