Page last updated: 2024-11-12

cryptophycin 52

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 CID9939639
CHEMBL ID316640
SCHEMBL ID12015033
MeSH IDM0294256

Synonyms (14)

Synonym
CHEMBL316640
cryptophycin-52
cryptophycin 52, (+)-
3-chloro-n-((2e,5s,6s)-5-hydroxy-1-oxo-6-((2r,3r)-3-phenyloxiranyl)-2-heptenyl)-o-methyl-d-tyrosyl-2,2-dimethyl-b-alanyl-2-hydroxy-4-methyl-pentanoic aicd (3-1)lactone, (2s)
cyclo(2,2-dimethyl-.beta.-alanyl-(2s)-2-hydroxy-4-methylpentanoyl-(2e,5s,6s)-5-hydroxy-6-((2r,3r)-3-phenyloxiranyl)-2-heptenoyl-3-chloro-o-methyl-d-tyrosyl)
pentanoic acid, 3-chloro-n-((2e,5s,6s)-5-hydroxy-1-oxo-6-((2r,3r)-3-phenyloxiranyl)-2-heptenyl)-o-methyl-d-tyrosyl-2,2-dimethyl-.beta.-alanyl-2-hydroxy-4-methyl-, (3,1)-lactone, (2s)-
cyclo(2,2-dimethyl-.beta.-alanyl-(2s)-2-hydroxy-4-methylpentanoyl-(2e,5s,6s)-5-hydroxy-6-((2r,3r)-3-phenyl-2-oxiranyl)-2-heptenoyl-3-chloro-o-methyl-d-tyrosyl)
(+)-cryptophycin 52
cryptophycin-52 [mi]
SCHEMBL12015033
(3s,10r,13e,16s)-10-[(3-chloro-4-methoxyphenyl)methyl]-6,6-dimethyl-3-(2-methylpropyl)-16-[(1s)-1-[(2r,3r)-3-phenyloxiran-2-yl]ethyl]-1,4-dioxa-8,11-diazacyclohexadec-13-ene-2,5,9,12-tetrone
LSXOBYNBRKOTIQ-RQUBOUMQSA-N
Q27280542
DTXSID201046100

Research Excerpts

Overview

Cryptophycin 52 is a synthetic derivative of Cryptophycin 1, a potent antimicrotubule agent isolated from cyanobacteria.

ExcerptReferenceRelevance
"Cryptophycin 52 is a synthetic derivative of Cryptophycin 1, a potent antimicrotubule agent isolated from cyanobacteria. "( A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
Al-Awar, RS; Andis, SL; Corbett, TH; Golakoti, T; Kennedy, JH; Liang, J; Moore, RE; Ray, JE; Schultz, RM; Subbaraju, GV, 2003
)
2.07
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID44346In vitro growth inhibitory activity in the human CCRF-CEM leukemia cell line.2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
AID120737Ratio of the median tumor weight in the treatment group over the median tumor weight in the control group on a schedule of 3-10 days and at a total dose of 32 mg/kg2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
AID88942Antiproliferative activity was evaluated by the 72 hr MTT cell viability assay using human colon carcinoma cells (GC3).1999Bioorganic & medicinal chemistry letters, Jan-04, Volume: 9, Issue:1
Synthesis and biological evaluation of novel cryptophycin analogs with modification in the beta-alanine region.
AID111305In vivo antitumor activity against murine pancreatic adenocarcinoma and measured as number of deaths on a schedule of 3-9 days and at a total dose of 42 mg/kg2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
AID1918879Cytotoxicity against human KB 3-1 cells assessed as reduction in cell viability2022Journal of natural products, 12-23, Volume: 85, Issue:12
Bioactive Arylnaphthalide Lignans from
AID111304In vivo antitumor activity against murine pancreatic adenocarcinoma and measured as number of deaths on a schedule of 3-10 days and at a total dose of 32 mg/kg2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
AID726203Cytotoxicity against human KB-3-1 cells by resazurin reduction assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Conjugates of modified cryptophycins and RGD-peptides enter target cells by endocytosis.
AID124782In vivo antitumor activity against murine pancreatic adenocarcinoma and measured as % weight loss on a schedule of 3-9 days and at a total dose of 42 mg/kg2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
AID224783Compound was tested for its antitumor activity in murine pancreatic adenocarcinoma PO3 model at the maximum tolerated dose(MTD)1999Bioorganic & medicinal chemistry letters, Jan-04, Volume: 9, Issue:1
Synthesis and biological evaluation of novel cryptophycin analogs with modification in the beta-alanine region.
AID120738Ratio of the median tumor weight in the treatment group over the median tumor weight in the control group on a schedule of 3-9 days and at a total dose of 42 mg/kg2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
AID124781In vivo antitumor activity against murine pancreatic adenocarcinoma and measured as % weight loss on a schedule of 3-10 days and at a total dose of 32 mg/kg2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
AID726202Cytotoxicity against human KBV1 cells by resazurin reduction assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Conjugates of modified cryptophycins and RGD-peptides enter target cells by endocytosis.
AID43714In vitro cytotoxicity against human leukemia CCRF-CEM cell line1999Bioorganic & medicinal chemistry letters, Feb-08, Volume: 9, Issue:3
Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region).
AID115257Log cell kill of tumor bearing mice on a schedule of 3-10 days and at a total dose of 32 mg/kg2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
A convergent approach to cryptophycin 52 analogues: synthesis and biological evaluation of a novel series of fragment a epoxides and chlorohydrins.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (40.00)18.2507
2000's1 (20.00)29.6817
2010's1 (20.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.57

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index20.57 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.57)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An Open Label, Randomized, Single Dose, 2-sequence, 2-period, Cross-over Phase 1 Study to Evaluate the Safety and Pharmacokinetics of AJU-C52H Compared to Coadministration of C52R1M With C52R2 in Healthy Adult Volunteers [NCT05077462]Phase 160 participants (Anticipated)Interventional2021-09-17Recruiting
An Open Label, Randomized, Single Dose, 2-sequence, 2-period, Cross-over Phase 1 Study to Evaluate the Safety and Pharmacokinetics of AJU-C52L Compared to Coadministration of C52R1H With C52R2 in Healthy Adult Volunteers [NCT05077475]Phase 160 participants (Anticipated)Interventional2021-09-24Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]