Page last updated: 2024-12-06

u 77779

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

Description

bizelesin: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID60794
CHEMBL ID284642
SCHEMBL ID4433
MeSH IDM0195836

Synonyms (27)

Synonym
bizelesin
nsc-615291
nsc615291
benzo[1,3-b']dipyrrol-4-ol, 6,6'-[carbonylbis(imino- 1h-indole-5,2-diylcarbonyl)]bis[8-(chloromethyl)-3,6,7,8-tetrahydro-1-methyl-, [s-(r*,r*)]
D03137
bizelesin (usan/inn)
1,3-bis(2-(((s)-1-(chloromethyl)-1,6-dihydro-5-hydroxy-8-methylbenzo(1,2-b:4,3-b')dipyrrol-3(2h)-yl)carbonyl)indol-5-yl)urea
u 77779
u-77779
bizelesin [usan:inn]
benzo(1,2-b:4,3-b')dipyrrol-4-ol, 6,6'-(carbonylbis(imino-1h-indole-5,2-diylcarbonyl))bis(8-(chloromethyl)-3,6,7,8-tetrahydro-1-methyl-, (s-(r*,r*))-
u-77,779
CHEMBL284642
1,3-bis[2-[(8s)-8-(chloromethyl)-4-hydroxy-1-methyl-7,8-dihydro-3h-pyrrolo[3,2-e]indole-6-carbonyl]-1h-indol-5-yl]urea
nsc 615291
unii-l0o9obi87e
l0o9obi87e ,
bizelesin [usan]
bizelesin [who-dd]
bizelesin [inn]
SCHEMBL4433
DTXSID00156213
DB12352
1,3-bis(2-((s)-1-(chloromethyl)-5-hydroxy-8-methyl-1,2,3,6-tetrahydropyrrolo[3,2-e]indole-3-carbonyl)-1h-indol-5-yl)urea
Q27282553
CS-0040330
HY-111397

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Preclinical animal studies have found bizelesin to be more toxic to beagle dogs than to rodents and that myelosuppression was the dose-limiting toxicity."( Myelotoxic effects of the bifunctional alkylating agent bizelesin on human, canine and murine myeloid progenitor cells.
Flora, KP; Garg, A; Grieshaber, CK; Murphy, MJ; Parchment, RE; Tomaszewski, JE; Volpe, DA, 1996
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID89265Cytotoxicity was determined after 1 hr exposure against six different human tumor cells lines2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Cytotoxic alpha-halogenoacrylic derivatives of distamycin A and congeners.
AID222135Antitumor activity against human colon CX-1 tumor Xenografts in Athymic mice at a dose of 7.81 micro g/kg2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3'-arylenebisacryloyl group as a linker.
AID233532Ratio between maximum dose within 10% body weight loss to tumor growth inhibition2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3'-arylenebisacryloyl group as a linker.
AID88790The myelotoxicity was tested in vitro on human granulocyte macrophage colony forming units (CFU-GM) cord blood derived hematopoietic cells (1 hr exposure)2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Cytotoxic alpha-halogenoacrylic derivatives of distamycin A and congeners.
AID90917Ratio between IC50 on human bone marrow progenitors (CFUGM) and tumor cells.2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
Cytotoxic alpha-halogenoacrylic derivatives of distamycin A and congeners.
AID139923Percentage change in body weight2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3'-arylenebisacryloyl group as a linker.
AID52839Compound was tested for antitumor activity against colon 26 murine adenocarcinoma infected CDF1 mice when administered at a dose of 15.6 ug/Kg intravenously1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
The novel cyclopropapyrroloindole(CPI) bisalkylators bearing methoxycarbonyl and trifluoromethyl groups.
AID222133Antitumor activity against human colon CX-1 tumor Xenografts in Athymic mice at a dose of 15.6 micro g/kg2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3'-arylenebisacryloyl group as a linker.
AID230241Ratio of MTD, maximum dose with in 10% body weight loss (ug/Kg) to that of TGI50 was reported1998Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15
The novel cyclopropapyrroloindole(CPI) bisalkylators bearing 3,3'-(1,4-phenylene)diacryloyl group as a linker.
AID87612Concentration required to inhibit the growth of HeLaS3 cells1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
The novel cyclopropapyrroloindole(CPI) bisalkylators bearing methoxycarbonyl and trifluoromethyl groups.
AID133224Percentage tumor growth inhibition as compared with the untreated group2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3'-arylenebisacryloyl group as a linker.
AID122178In vitro antitumor activity against colon 26 murine adenocarcinoma in male CDF1 mice and was expressed as 50% tumor growth inhibition.1998Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15
The novel cyclopropapyrroloindole(CPI) bisalkylators bearing 3,3'-(1,4-phenylene)diacryloyl group as a linker.
AID87609In vitro cytotoxicity against HeLaS3 human uterine cervix carcinoma1998Bioorganic & medicinal chemistry letters, Aug-04, Volume: 8, Issue:15
The novel cyclopropapyrroloindole(CPI) bisalkylators bearing 3,3'-(1,4-phenylene)diacryloyl group as a linker.
AID87605Inhibitory activity against HeLaS3 human uterine cervix carcinoma cells2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Novel seco cyclopropa[c]pyrrolo[3,2-e]indole bisalkylators bearing a 3,3'-arylenebisacryloyl group as a linker.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's23 (56.10)18.2507
2000's17 (41.46)29.6817
2010's1 (2.44)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (4.76%)5.53%
Reviews4 (9.52%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other36 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]