Page last updated: 2024-11-07

sn 38

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

Description

SN-38 : A member of the class of pyranoindolizinoquinolines that is (4S)-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione bearing two additional ethyl substituents at positions 4 and 11 as well as two additional hydroxy substituents at positions 4 and 9. It is the active metabolite of irinotecan and is ~1000 times more active than irinotecan itself. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID104842
CHEBI ID8988
SCHEMBL ID34018
MeSH IDM0147536

Synonyms (83)

Synonym
AC-1357
NCI60_026056
avachem1025
1h-pyrano[3',7]indolizino[1,2-b]quinoline- 3,14(4h,12h)-dione, 4,11-diethyl-4,9-dihydroxy-, (4s)-
7-ethyl-10-hydroxycamptothecin ,
sn 38
nsc-673596
7-ethyl-10-hydroxy-20(s)-camptothecin
(4s)-4,11-diethyl-4,9-dihydroxy-1h-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4h,12h)-dione
captothecin, 7-ethyl-10-hydroxy-
sn-38
86639-52-3
sn38
nsc673596
diethyl(dihydroxy)[?]dione
1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione, 4,11-diethyl-4,9-dihydroxy-, (4s)-
7-ethyl-10-hydroxy-20(s)-cpt
NCGC00167831-01
(4s)-4,11-diethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione
7-ethyl-10-hydroxy-20(s)-campthothecin
E0748
chebi:8988 ,
camptothecin, 7-ethyl-10-hydroxy-
nk-012
it-141
nk 012
nk012
110714-48-2
BCP9000200
(+)-7-ethyl-10-hydroxycamptothecin
AKOS015920433
c22h20n2o5
bdbm50418088
h-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4h,12h)-dione, 4,11-diethyl-4,9-dihydroxy-, (s)-
0h43101t0j ,
le-sn38
10-hydroxy-7-ethylcamptothecin
sn 38 lactone
unii-0h43101t0j
(4s)-4,11-diethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)dione
1h-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4h,12h)-dione, 4,11-diethyl-4,9-dihydroxy-, (4s)-
s-(+)-7-ethyl-10-hydroxycampothecin
sn 38 [who-dd]
S4908
(19s)-10,19-diethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2(11),3,5,7,9,15(20)-heptaene-14,18-dione
gtpl6925
DB05482
HY-13704
CS-1579
SCHEMBL34018
(s)-4,11-diethyl-4,9-di-oh-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione
mfcd00871873
(s)-4,11-diethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione
Q-100871
DTXSID4040399
(4s)-4,11-diethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)dione, aldrichcpr
EX-A989
7-ethyl-10-hydroxycamptothecin, >=98% (hplc), powder
HMS3652P12
NCGC00167831-05
sn-38(nk-012)
7-ethyl-10-hydroxycamptothecin ((s)-4,11-diethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione)
SW219948-1
113015-38-6
(19s)-10,19-diethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaene-14,18-dione
10-hydroxy-7-ethyl-camptothecin
FJHBVJOVLFPMQE-QFIPXVFZSA-N
10-hydroxy-7-ethyl camptothecin
HMS3677B12
AS-13533
BCP01386
HMS3413B12
Q1750127
EN300-122379
(19s)-10,19-diethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2(11),3,5,7,9,15(20)-heptaene-14,18-dione
CCG-264764
rs4 ,
BP-24513
A857464
(4s)-4,9-dihydroxy-4,11-diethyl-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione;sn-38
sn 38- bio-x
BE164132
Z1541759909

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In xenograft models, 9a demonstrated significant activity without overt adverse effects at 5 and 10 mg/kg, comparable to 3 at 100 mg/kg."( Design, synthesis, mechanisms of action, and toxicity of novel 20(s)-sulfonylamidine derivatives of camptothecin as potent antitumor agents.
Chang, LC; Goto, M; Hung, HY; Kuo, DH; Kuo, SC; Lee, KH; Liu, YQ; Morris-Natschke, SL; Nan, X; Pan, SL; Qian, K; Teng, CM; Wang, CY; Wang, MJ; Wu, TS; Wu, YC; Yang, JS; Yang, L; Yang, XM; Zhao, XB; Zhao, YL, 2014
)
0.4

Bioavailability

ExcerptReferenceRelevance
" On the basis of plasma concentrations of compound 1 and SN38 (14), the oral bioavailability of compound 3a and 15 in beagle dogs was found to be 97."( Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle.
Chu, H; Gao, Q; Gong, A; Huang, Q; Huang, X; Lei, B; Li, P; Li, Y; Liao, P; Liu, J; Lu, Y; Luo, X; Ni, J; Qian, G; Qin, L; Qiu, G; Tang, P; Wei, Y; Yan, P; Yu, Y; Zhang, C; Zhang, X; Zheng, S; Zhou, Y; Zhu, G, 2017
)
0.46
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
EC 5.99.1.2 (DNA topoisomerase) inhibitorA topoisomerase inhibitor that inhibits the bacterial enzymes of the DNA topoisomerases, Type I class (EC 5.99.1.2) that catalyze ATP-independent breakage of one of the two strands of DNA, passage of the unbroken strand through the break, and rejoining of the broken strand. These bacterial enzymes reduce the topological stress in the DNA structure by relaxing negatively, but not positively, supercoiled DNA.
drug metabolitenull
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
pyranoindolizinoquinoline
delta-lactoneA lactone having a six-membered lactone ring.
tertiary alcoholA tertiary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has three other carbon atoms attached to it.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (5)

PathwayProteinsCompounds
Irinotecan Pathway, Pharmacodynamics141
Irinotecan Action Pathway2411
Irinotecan Metabolism Pathway2411
Irinotecan Pathway, Pharmacokinetics172
Irinotecan pathway05

Protein Targets (18)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency3.54815.623417.292931.6228AID485281
Fumarate hydrataseHomo sapiens (human)Potency0.00370.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency1.17090.00529.466132.9993AID1347411
EWS/FLI fusion proteinHomo sapiens (human)Potency0.10600.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
polyproteinZika virusPotency0.00370.00308.794948.0869AID1347053
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency0.35480.00798.23321,122.0200AID2546
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency1.77830.251215.843239.8107AID504327
Interferon betaHomo sapiens (human)Potency1.17090.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cytochrome P450 3A4Homo sapiens (human)Ki26.00000.00011.41629.9000AID589114
DNA topoisomerase 1Homo sapiens (human)IC50 (µMol)3.25000.02101.862610.0000AID1708533; AID418336
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)IC50 (µMol)360.00000.30003.25807.3000AID1222388
DNA topoisomerase 1Mus musculus (house mouse)IC50 (µMol)4.00004.00004.00004.0000AID211118
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)0.17600.00401.966610.0000AID679628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA topoisomerase 1Homo sapiens (human)EC50 (µMol)0.19500.05000.33592.0150AID240049
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
UDP-glucuronosyltransferase 1A9Homo sapiens (human)Km13.00005.00006.830010.0000AID624637
DNA topoisomerase 1Homo sapiens (human)CC500.80000.80001.20293.2000AID56562
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km24.50004.49006.51339.0000AID1222390; AID624630
UDP-glucuronosyltransferase 1A4Homo sapiens (human)Km147.00007.00007.00007.0000AID624633
UDP-glucuronosyltransferase 2B15Homo sapiens (human)Km186.00007.00007.00007.0000AID624638
UDP-glucuronosyltransferase 1A7Homo sapiens (human)Km5.00005.00007.20009.4000AID624635
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)Km4.00004.00005.40006.8000AID682062
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (93)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A9Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A9Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A9Homo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
DNA topological changeDNA topoisomerase 1Homo sapiens (human)
chromatin remodelingDNA topoisomerase 1Homo sapiens (human)
circadian rhythmDNA topoisomerase 1Homo sapiens (human)
response to xenobiotic stimulusDNA topoisomerase 1Homo sapiens (human)
programmed cell deathDNA topoisomerase 1Homo sapiens (human)
phosphorylationDNA topoisomerase 1Homo sapiens (human)
peptidyl-serine phosphorylationDNA topoisomerase 1Homo sapiens (human)
circadian regulation of gene expressionDNA topoisomerase 1Homo sapiens (human)
embryonic cleavageDNA topoisomerase 1Homo sapiens (human)
chromosome segregationDNA topoisomerase 1Homo sapiens (human)
DNA replicationDNA topoisomerase 1Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1-6Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1-6Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
acute-phase responseUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to nutrientUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
animal organ regenerationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to lipopolysaccharideUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
response to starvationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
negative regulation of steroid metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
biphenyl catabolic processUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to ethanolUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to glucocorticoid stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cellular response to estradiol stimulusUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
bilirubin conjugationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
heme catabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A4Homo sapiens (human)
vitamin D3 metabolic processUDP-glucuronosyltransferase 1A4Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B15Homo sapiens (human)
steroid metabolic processUDP-glucuronosyltransferase 2B15Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B15Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B15Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
coumarin metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
retinoic acid metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
flavone metabolic processUDP-glucuronosyltransferase 1A7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
flavonoid glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
xenobiotic glucuronidationUDP-glucuronosyltransferase 1A7Homo sapiens (human)
liver developmentUDP-glucuronosyltransferase 1A7Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (56)

Processvia Protein(s)Taxonomy
retinoic acid bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A9Homo sapiens (human)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingDNA topoisomerase 1Homo sapiens (human)
DNA bindingDNA topoisomerase 1Homo sapiens (human)
chromatin bindingDNA topoisomerase 1Homo sapiens (human)
double-stranded DNA bindingDNA topoisomerase 1Homo sapiens (human)
single-stranded DNA bindingDNA topoisomerase 1Homo sapiens (human)
RNA bindingDNA topoisomerase 1Homo sapiens (human)
DNA topoisomerase type I (single strand cut, ATP-independent) activityDNA topoisomerase 1Homo sapiens (human)
protein serine/threonine kinase activityDNA topoisomerase 1Homo sapiens (human)
protein bindingDNA topoisomerase 1Homo sapiens (human)
ATP bindingDNA topoisomerase 1Homo sapiens (human)
DNA binding, bendingDNA topoisomerase 1Homo sapiens (human)
protein domain specific bindingDNA topoisomerase 1Homo sapiens (human)
supercoiled DNA bindingDNA topoisomerase 1Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1-6Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1-6Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1-6Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
steroid bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A4Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B15Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B15Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
enzyme inhibitor activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein kinase C bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
enzyme bindingUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein homodimerization activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein heterodimerization activityUDP-glucuronosyltransferase 1A7Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Processvia Protein(s)Taxonomy
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A9Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A9Homo sapiens (human)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
nuclear chromosomeDNA topoisomerase 1Homo sapiens (human)
P-bodyDNA topoisomerase 1Homo sapiens (human)
fibrillar centerDNA topoisomerase 1Homo sapiens (human)
male germ cell nucleusDNA topoisomerase 1Homo sapiens (human)
nucleusDNA topoisomerase 1Homo sapiens (human)
nucleoplasmDNA topoisomerase 1Homo sapiens (human)
nucleolusDNA topoisomerase 1Homo sapiens (human)
perikaryonDNA topoisomerase 1Homo sapiens (human)
protein-DNA complexDNA topoisomerase 1Homo sapiens (human)
nucleolusDNA topoisomerase 1Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1-6Homo sapiens (human)
intracellular membrane-bounded organelleUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1-6Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
plasma membraneUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
perinuclear region of cytoplasmUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulum chaperone complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
cytochrome complexUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A1 Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A4Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B15Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A7Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 1A7Homo sapiens (human)
endoplasmic reticulumUDP-glucuronosyltransferase 1A7Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (414)

Assay IDTitleYearJournalArticle
AID1347110qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347119qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347109qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347118qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347126qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347115qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347113qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347128qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347125qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347116qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347127qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347129qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347123qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347122qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347111qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347112qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347121qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347114qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347117qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347124qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1470601Cytotoxicity against human HT-29 cells pretreated for 24 hrs under normoxic condition followed by compound washout measured after 72 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID1593650Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives.
AID1703229Solubility of compound in phosphate buffer at pH 7.4 incubated for 24 hrs under shaking condition by HPLC analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID249952In vitro cytotoxic activity against human RPM12650 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1666200Cytotoxicity against human 16HBE cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging.
AID1655976Cytotoxicity against human SK-MEL-24 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1.
AID666765Inhibition of topo 1-mediated relaxation of supercoiled pBR322 at 10 to 100 uM after 30 mins using ethidium bromide by agarose-gel electrophoresis2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and biological evaluation of new homocamptothecin analogs.
AID624633Drug glucuronidation reaction catalyzed by human recombinant UGT1A42005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID249906In vitro cytotoxic activity against human T24 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID624638Drug glucuronidation reaction catalyzed by human recombinant UGT2B152005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1708532Growth inhibition of human NCI-H226 cells by Cell-titer96 assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID321558Antiproliferative activity against human DU145 cells after 96 hrs2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and bioevaluation of 22-hydroxyacuminatine analogs.
AID624630Drug glucuronidation reaction catalyzed by human recombinant UGT1A12005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID84434Antiproliferative activity against human HT-29 colon cell line1999Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II.
AID1215101Terminal elimination rate constant in cancer patient normal renal function administered as infusion after 0.25 to 1.5 hrs by RP-HPLC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Delayed elimination of SN-38 in cancer patients with severe renal failure.
AID249937In vitro cytotoxic activity against human Hs 174.T cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1626189Synergistic cytotoxicity in human HT-29 cells assessed as dose reduction index ratio in presence of CoCl2-induced hypoxic conditions measured at 80 % cell growth inhibition after 72 hrs in presence of compound-5c by cell counter method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.
AID247883Concentration required to inhibit growth of human prostate PC-3 carcinoma cell line2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
AID216612Antitumor activity against MTW0 WiDr xenografts in nude mice at a dose of 10 umol/kg2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID679163TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cell2005Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.
AID414759Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents.
AID589114Mechanism based inhibition of human cytochrome P450 3A42005Current drug metabolism, Oct, Volume: 6, Issue:5
Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
AID248673In-vitro inhibitory concentration for human tumor HELA cell-line was determined using MTT assay after 3 days of incubation2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Synthesis and antitumor activity of the hexacyclic camptothecin derivatives.
AID418333Antiproliferative activity against human NCI-H460 cells after 3 days2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Synthesis of new camptothecin analogs with improved antitumor activities.
AID679412TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.10uL/oocyte in Xenopus laevis oocytes2005Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.
AID1194773Stability in human plasma assessed as lactone moieties level at 1 uM incubated at 37 degC after 3 hrs by HPLC method2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents.
AID1754555Cytotoxicity against human CCD-841CoN cells assessed as inhibition of cell growth measured after 72 hrs2021Bioorganic & medicinal chemistry letters, 08-15, Volume: 46New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology.
AID679173TP_TRANSPORTER: drug resistance in BCRP-expressing K562 cells2003Molecular cancer therapeutics, Jan, Volume: 2, Issue:1
Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists.
AID249916In vitro cytotoxic activity against human T98G cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249935In vitro cytotoxic activity against human HT144 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID26144Half-life in PBS buffer solution in the absence of human serum albumin1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID745327Cytotoxicity against human DU145 cells2013European journal of medicinal chemistry, May, Volume: 63Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents.
AID28882Half life of compound in PBS suspension2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID1222390Drug metabolism assessed as UGT1A1 (unknown origin)-mediated compound glucuronidation2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors.
AID1754554Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs2021Bioorganic & medicinal chemistry letters, 08-15, Volume: 46New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology.
AID680997TP_TRANSPORTER: inhibition of E1S uptake by 7-ethyl-10-hydroxycamptothecin at a concentration of 20uM in membrane vesicle from BCRP-expressing K562 cells2003Molecular pharmacology, Sep, Volume: 64, Issue:3
Breast cancer resistance protein exports sulfated estrogens but not free estrogens.
AID426062Antitumor activity against human A549/ATCC cells by SRB method2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation.
AID321560Antiproliferative activity against human HT29 cells after 96 hrs2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and bioevaluation of 22-hydroxyacuminatine analogs.
AID1465633Cmax in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle.
AID678965TP_TRANSPORTER: drug resistance in BCRP-expressing PA317 cells2003International journal of cancer, Dec-10, Volume: 107, Issue:5
Single amino acid substitutions in the transmembrane domains of breast cancer resistance protein (BCRP) alter cross resistance patterns in transfectants.
AID749703Inhibition of HDAC6 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1561988Drug uptake in human A549 cells assessed as blue fluorescence at 5 uM after 12 hrs by confocal laser scanning microscopic analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID678800TP_TRANSPORTER: increase of cytotoxicity by GF120918 in MX3 cells2001Clinical cancer research : an official journal of the American Association for Cancer Research, Apr, Volume: 7, Issue:4
Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.
AID1703210Cytotoxicity against human A549 assessed as reduction in cell viability measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID1386601Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay2018Journal of natural products, 09-28, Volume: 81, Issue:9
Flabellipparicine, a Flabelliformide-Apparicine-Type Bisindole Alkaloid from Tabernaemontana divaricata.
AID249946In vitro cytotoxic activity against human Capan-2 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID247623Inhibitory concentration against human HCT116 colon cancer cell line2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
AID249956In vitro cytotoxic activity against human Su.86.86 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1561986Drug uptake in human A549 cells assessed as blue shift in absorption spectrum at 5 uM by UV-visible absorption spectral analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID28493% lactone at different intervals of time in PBS with RBC suspension2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID594370Cytotoxicity against human A549 cells2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Semisynthesis of triptolide analogues: effect of γ-lactone and C-14 substituents on cytotoxic activities.
AID27450Half-life period in human plasma1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID1708541Resistance index, ratio of GI50 for growth inhibition of ARC-111-resistant human HA6n cells to GI50 for growth inhibition of human HCT-116 cells2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID1076087Cytotoxicity against human HCT116 cells2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.
AID227859In Vitro cytotoxicity against human stomach cancer cell line (MKN45)2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID26145Half-life in PBS buffer solution in the presence of human serum albumin1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID1294917Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB assay2016European journal of medicinal chemistry, Jun-30, Volume: 11610-Boronic acid substituted camptothecin as prodrug of SN-38.
AID27446Half-life period in HSA buffer at 37 C in the presence of human serum albumin1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID1515334Antiproliferative activity against human U251 cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID234607Tested for (median survival time of treated/control animals) x100 at dosage of 30 mg/kg.1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues.
AID1655974Cytotoxicity against human C3PV cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1.
AID679982TP_TRANSPORTER: intracellular accumulation in KB-3-1 and MRP1-expressing KB-3-1 cells1999Molecular pharmacology, May, Volume: 55, Issue:5
ATP-Dependent efflux of CPT-11 and SN-38 by the multidrug resistance protein (MRP) and its inhibition by PAK-104P.
AID1386602Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay2018Journal of natural products, 09-28, Volume: 81, Issue:9
Flabellipparicine, a Flabelliformide-Apparicine-Type Bisindole Alkaloid from Tabernaemontana divaricata.
AID269202Inhibition of human H460 cell growth2006Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17
Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID249947In vitro cytotoxic activity against human HT1197 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1593649Cytotoxicity against human TE8 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives.
AID624635Drug glucuronidation reaction catalyzed by human recombinant UGT1A72005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID249948In vitro cytotoxic activity against human U-373MG cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID28876Half life for of compound in PBS with RBC suspension2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID249921In vitro cytotoxic activity against human A-704 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID222931Association constant for the binding of lactone form to human serum albumin1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID249931In vitro cytotoxic activity against human AL-12T cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1294916Cytotoxicity against human HCT15 cells assessed as growth inhibition after 72 hrs by SRB assay2016European journal of medicinal chemistry, Jun-30, Volume: 11610-Boronic acid substituted camptothecin as prodrug of SN-38.
AID56562Cytotoxicity against DNA topoisomerase I purified from calf thymus1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity.
AID1194768Cytotoxicity against human HT-29 cells after 72 hrs by sulforhodamine B assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents.
AID679628TP_TRANSPORTER: drug resistance(Imatinib mesylate) in BCRP-expressing SaoS2 cells2004Cancer research, Apr-01, Volume: 64, Issue:7
Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro.
AID1470605Selectivity ratio of IC50 for human NCI-H460 cells under normoxic condition to IC50 for human NCI-H460 cells under hypoxic condition2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID1470602Selectivity ratio of IC50 for human HT-29 cells under normoxic condition to IC50 for human HT-29 cells under hypoxic condition2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID249954In vitro cytotoxic activity against human SK-UT-1B cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID679413TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.10uL/oocyte in Xenopus laevis oocytes2004Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity.
AID216617Relative tumor growth (RTG), calculated by dividing MTW28 by that on day 0 (MTW0) against WiDr xenografts in nude mice at a dose of 10 umol/kg2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1708540Growth inhibition of ARC-111-resistant human HA6n cells by Cell-titer96 assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID418335Antiproliferative activity against human PC6 cells carrying pRC after 6 days2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Synthesis of new camptothecin analogs with improved antitumor activities.
AID202842Antiproliferative activity against human SKOV-3 ovarian cell line1999Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II.
AID219146In Vitro cytotoxicity against human breast cancer cell line (SK-BR-3)2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1488981Selectivity ratio, IC50 for human H460 cells under normoxic condition to IC50 for human H460 cells under hypoxic condition2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole.
AID1399559Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
A series of camptothecin prodrugs exhibit HDAC inhibition activity.
AID249941In vitro cytotoxic activity against human Panc-1 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID146690Cytotoxicity against human non-small-cell lung carcinoma cell line H460 (NSCLC-H460)2001Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20
Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID216615Percentage of inhibition rate (IR) against WiDr xenografts in nude mice at a dose of 10 umol/kg2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID680750TP_TRANSPORTER: inhibition of E1S uptake (SN38 10 u M) in OATP1B1-expressing HEK293 cells2005Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.
AID222926% of lactone form at equilibrium in PBS buffer at 37 C in the absence of human serum albumin1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID548079Growth inhibition of human lung cancer cells after 72 hrs by sulforhodamine B assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and antitumor activity of novel benzimidazole-5-carboxylic acid derivatives and their transition metal complexes as topoisomerease II inhibitors.
AID346586Induction of human recombinant topoisomerase 1-mediated SV40 DNA cleavage at 1 to 50 uM after 30 mins by PAGE2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Semisynthesis, biological activity, and molecular modeling studies of C-ring-modified camptothecins.
AID234776Tested for (median survival time of treated/control animals) x100 at dosage of 60 mg/kg.1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues.
AID131159Effect in increasing life span of mice bearing L1210 leukemia1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity.
AID240049Effective concentration against DNA topoisomerase I2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
AID1222389Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors.
AID679172TP_TRANSPORTER: drug resistance in BCRP-expressing LLC-PK1 cells2003Molecular pharmacology, Sep, Volume: 64, Issue:3
Breast cancer resistance protein exports sulfated estrogens but not free estrogens.
AID332046Cytotoxicity against human H460 cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
Synthesis and cytotoxic activity of new 9-substituted camptothecins.
AID749702Inhibition of HDAC8 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1215100Terminal elimination rate constant in cancer patient with severe renal failure administered as infusion after 0.25 to 1.5 hrs by RP-HPLC analysis2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Delayed elimination of SN-38 in cancer patients with severe renal failure.
AID418342Ratio of IC50 for human PC6 expressing BCRP cells to IC50 for human PC6 cells carrying pRC2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Synthesis of new camptothecin analogs with improved antitumor activities.
AID1535491Solubility of the compound in phosphate buffered saline by UV-spectroscopic analysis2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
Monodisperse oligoethylene glycols modified Camptothecin, 10-Hydroxycamptothecin and SN38 prodrugs.
AID1703223Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells level at 0.001 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.17%)2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID249917In vitro cytotoxic activity against human WiDr cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1428729Drug excretion in human urine upto 48 hrs2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
The long story of camptothecin: From traditional medicine to drugs.
AID679165TP_TRANSPORTER: inhibition of Estrone-3-sulfate uptake(Estrone-3-sulfate: 9.2nM) in Xenopus laevis oocytes2005Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.
AID133755Maximally tolerated dose in mice bearing L1210 leukemia.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity.
AID1294919Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay2016European journal of medicinal chemistry, Jun-30, Volume: 11610-Boronic acid substituted camptothecin as prodrug of SN-38.
AID1593647Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives.
AID1900082Cytotoxicity against human A549 cells assessed as cell growth inhibition incubated for 120 hrs by CCK-8 assay2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency
AID1708528Growth inhibition of human Hep3B cells by Cell-titer96 assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID680206TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.09uL/oocyte in Xenopus laevis oocytes2005Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.
AID249951In vitro cytotoxic activity against human NCI-H727 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1703226Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells level at 1 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.07%)2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID245827Percent tumor-weight inhibition in mouse tumor sarcoma-180 model after intraperitoneal administration of 5 mg/kg dose in comparison with control mice2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
AID1708534Inhibition of human topoisomerase 1 assessed as stabilization of Topl-DNA cleavable complex by measuring band intensity of free Top-l at 0.1 to 1 uM by band-depletion assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID249960In vitro cytotoxic activity against human MCF7HTB-22 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249911In vitro cytotoxic activity against human FaDu cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1515352Antiproliferative activity against human LOXIMVI cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID380253Inhibition of topoisomerase 1-mediated SV40 DNA cleavage at 1 to 50 uM by gel electrophoresis2006Journal of natural products, Dec, Volume: 69, Issue:12
Cucurbitane triterpenes from the fruiting bodies and cultivated mycelia of Leucopaxillus gentianeus.
AID28494% lactone at different intervals of time in human blood.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID1488982Selectivity ratio, IC50 for human HT-29 cells under normoxic condition to IC50 for human HT29 cells under hypoxic condition2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole.
AID1076086Cytotoxicity against human A549 cells2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.
AID247882Concentration required to inhibit growth of human cervical HeLa carcinoma cell line2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
AID83623In vitro inhibitory concentration required against HT-29 human colon cancer cells2003Bioorganic & medicinal chemistry letters, Mar-10, Volume: 13, Issue:5
Cancer chemotherapy: a SN-38 (7-ethyl-10-hydroxycamptothecin) glucuronide prodrug for treatment by a PMT (Prodrug MonoTherapy) strategy.
AID1515357Antiproliferative activity against human SKOV3 cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID91475Binding parameter of the carboxylate form to human serum albumin; n value1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID1900088Dissociation constant pKa of the compound2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency
AID1561995Cytotoxicity agains human HL7702 cells assessed as reduction in cell viability after 72 hrs by SRB assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID249955In vitro cytotoxic activity against human SKMEL-28 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1815775Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
The BASHY Platform Enables the Assembly of a Fluorescent Bortezomib-GV1001 Conjugate.
AID612419Stimulation of human recombinant DNA topoisomerase 1-mediated 751-bp BamHI-EcoRV fragment of SV40 DNA cleavage at 1 to 50 uM after 30 mins by polyacrylamide gel-electrophoresis2011Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16
Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D.
AID234603Tested for (median survival time of treated/control animals) x100 at dosage of 120 mg/kg.1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues.
AID249923In vitro cytotoxic activity against human DLD-1 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID594371Cytotoxicity against human HT-29 cells2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Semisynthesis of triptolide analogues: effect of γ-lactone and C-14 substituents on cytotoxic activities.
AID249933In vitro cytotoxic activity against human CAKI-2 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1515359Antiproliferative activity against human ACHN cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID249950In vitro cytotoxic activity against human MALME-3M cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID237674Half life of compound for DNA topoisomerase I complex was determined2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
AID1561993Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability after 72 hrs by SRB assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID222929n value for the binding of lactone form to human serum albumin (n value = number of amino acid per binding site)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID249918In vitro cytotoxic activity against human 769-P cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID680548TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.16uL/oocyte in Xenopus laevis oocytes2005Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.
AID1666201Cytotoxicity against FR-negative human A549 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging.
AID1593653Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives.
AID1294921Cytotoxicity against human U251 cells assessed as growth inhibition after 72 hrs by SRB assay2016European journal of medicinal chemistry, Jun-30, Volume: 11610-Boronic acid substituted camptothecin as prodrug of SN-38.
AID1708529Growth inhibition of human SJRH30 cells by Cell-titer96 assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID249940In vitro cytotoxic activity against human MES-SA cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID411092Cytotoxicity against human A549 cells by SRB method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin.
AID1515344Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID1076083Cytotoxicity against human HT-29 cells assessed as growth inhibition after 3 days by SRB assay2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.
AID745328Cytotoxicity against human HT-29 cells2013European journal of medicinal chemistry, May, Volume: 63Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents.
AID249905In vitro cytotoxic activity against human C32 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID244702Percent change in body-weight of mouse tumor sarcoma-180 model after intraperitoneal administration of 5 mg/kg dose2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
AID1541742Cytotoxicity against human HeLa cells assessed as cell death at 10 uM after 24 hrs by MTT assay2020ACS medicinal chemistry letters, Jan-09, Volume: 11, Issue:1
Mitochondrial Impairment by Cyanine-Based Small Molecules Induces Apoptosis in Cancer Cells.
AID150520In vitro antitumor activity against P388 (murine leukemia) cells.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues.
AID1561994Antiproliferative activity against human Capan1 cells assessed as reduction in cell viability after 72 hrs by SRB assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID346585Antiproliferative activity against human NCI-H460 cells after short term exposure for 1 hr measured after 72 hrs in drug-free medium2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
Semisynthesis, biological activity, and molecular modeling studies of C-ring-modified camptothecins.
AID223634In Vitro cytotoxicity against human ovarian cancer cell line (SK-OV-3)2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1201344Inhibition of human recombinant topoisomerase 1-dependent DNA cleavage using 751-bp BamHI-EcoRI fragment of SV40 DNA at 50 uM incubated for 30 mins by PAGE method2015European journal of medicinal chemistry, Apr-13, Volume: 94Water-soluble isoindolo[2,1-a]quinoxalin-6-imines: in vitro antiproliferative activity and molecular mechanism(s) of action.
AID249949In vitro cytotoxic activity against human ZR-75-1 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID680556TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cells2005Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 33, Issue:3
Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.
AID1222394Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation using 4 to 75 uM estradiol by LC-MS/MS method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors.
AID414758Cytotoxicity against human KB3-1 cells after 4 days by MTT method2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents.
AID221332In Vitro cytotoxicity against human lung cancer cell line (A549)2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID216613Antitumor activity against MTW28 WiDr xenografts in nude mice at a dose of 10 umol/kg2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1703222Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells level at 0.001 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.07%)2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID1703230Solubility of compound in water incubated for 24 hrs under shaking condition by HPLC analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID1222388Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method2011Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2
Correlation between bilirubin glucuronidation and estradiol-3-gluronidation in the presence of model UDP-glucuronosyltransferase 1A1 substrates/inhibitors.
AID1488979Cytotoxicity against human HT-29 cells assessed as growth reduction under normoxic condition after 72 hrs by MTT assay2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole.
AID680984TP_TRANSPORTER: inhibition of accumulation by antisense of BCRP in PC-6/SN2-5,PC-6/SN2-5H cells2001Biochemical and biophysical research communications, Feb-09, Volume: 280, Issue:5
Breast cancer resistance protein directly confers SN-38 resistance of lung cancer cells.
AID1562010Inhibition of topoisomerase 1 in human A549 cells assessed as increase in phosphorylated KAP1 expression at 0.04 uM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID1703213Cytotoxicity against human COLO 205 assessed as reduction in cell viability measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID681563TP_TRANSPORTER: Cytotoxicity in MT-4 and MT-4/DOX500 cells2003Molecular pharmacology, Jan, Volume: 63, Issue:1
Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors.
AID222924% of lactone form at equilibrium in HSA buffer at 37 C in the presence of human serum albumin1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID1900084Cytotoxicity against HEK293T cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency
AID1515366Antiproliferative activity against human DU145 cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID1754553Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs2021Bioorganic & medicinal chemistry letters, 08-15, Volume: 46New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology.
AID55802Antiproliferative activity against human DU145 prostate cell line1999Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II.
AID1708526Growth inhibition of human MDA-MB-231 cells by Cell-titer96 assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID249908In vitro cytotoxic activity against human A427 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1561991Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID249914In vitro cytotoxic activity against human LoVo cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID248674In-vitro inhibitory concentration for human tumor HL60 cell-line was determined using SRB assay after 3 days of incubation2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Synthesis and antitumor activity of the hexacyclic camptothecin derivatives.
AID331823Antiproliferative activity against human H460 cells after 1 hr of drug exposure measured after 72 hrs2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.
AID242837Stability constant for DNA topoisomerase I complex in competitive DNA assay2004Bioorganic & medicinal chemistry letters, Nov-01, Volume: 14, Issue:21
Camptothecin analogs with bulky, hydrophobic substituents at the 7-position via a Grignard reaction.
AID163143Tested in vitro for the inhibition of QG-56 (human lung squamous cell carcinoma) cell line by MTT assay1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues.
AID1561999Induction of cell cycle arrest in human A549 cells at 3 to 10 nM after 24 hrs by RNase A/PI-staining based flow cytometric analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID253444Lethal toxicity against mouse tumor sarcoma-180 model after intraperitoneal administration of 5 mg/kg dose expressed as number of deaths out of 10 mice2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
AID1666195Cytotoxicity against FR-positive human SKHEP1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging.
AID249957In vitro cytotoxic activity against human MiaPaca-2 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1194769Inhibition of topoisomerase 1 (unknown origin) at 100 uM using supercoiled pBR322 DNA substrate by ethidium bromide staining based electrophoresis method2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents.
AID1562000Induction of cell cycle arrest in human HCT116 cells at 3 nM after 24 hrs by RNase A/PI-staining based flow cytometric analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID1703216Cytotoxicity against human NCI-H1975 assessed as reduction in cell viability measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID426063Antitumor activity against human HT-29 cells by SRB method2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation.
AID1703225Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells level at 0.03 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.17%)2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID216614Percentage of complete regression (CR) against WiDr xenografts in nude mice at a dose of 10 umol/kg2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1488977Cytotoxicity against human NCI-H460 cells assessed as growth reduction under normoxic condition after 72 hrs by MTT assay2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole.
AID249919In vitro cytotoxic activity against human 786-O cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1294922Inhibition of topoisomerase 1 (unknown origin) assessed as reduction in enzyme-mediated relaxation of supercoiled pBR322 DNA at 100 uM after 30 mins by agarose gel electrophoresis2016European journal of medicinal chemistry, Jun-30, Volume: 11610-Boronic acid substituted camptothecin as prodrug of SN-38.
AID91477Association constant for the binding of the carboxylate form to human serum albumin;(M aa)e-11994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID1703214Cytotoxicity against human Raji assessed as reduction in cell viability measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID1515363Antiproliferative activity against human MKN28 cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID1708527Growth inhibition of human HCT-116 cells by Cell-titer96 assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID249907In vitro cytotoxic activity against human A204 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID234605Tested for (median survival time of treated/control animals) x100 at dosage of 240 mg/kg.1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues.
AID1470603Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID690722Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Camptothecins in tumor homing via an RGD sequence mimetic.
AID745329Inhibition of topoisomerase 1 (unknown origin)-mediated DNA cleavage at 1 uM relative to SN-382013European journal of medicinal chemistry, May, Volume: 63Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents.
AID222928n value for the binding of carboxylate form to human serum albumin (n value = number of amino acid per binding site)1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID1561992Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID1708530Growth inhibition of human A498 cells by Cell-titer96 assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID249936In vitro cytotoxic activity against human HT1080 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1190166Cytotoxicity against drug-resistant human S1-M1-80 cells expressing ABCG2 G482 mutant after 72 hrs by MTT assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
IND-2, a pyrimido[1″,2″:1,5]pyrazolo[3,4-b]quinoline derivative, circumvents multi-drug resistance and causes apoptosis in colon cancer cells.
AID1561987Drug uptake in human A549 cells assessed as maximum emission peaks at 430 nm at 5 uM by fluorescence emission spectral analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID749704Inhibition of HDAC1 in human HeLa cells using Fluor-de-Lys as substrate after 15 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID249953In vitro cytotoxic activity against human SK-LMS-1 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID418331Antiproliferative activity against human HCT116 cells after 3 days2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Synthesis of new camptothecin analogs with improved antitumor activities.
AID248707In-vitro inhibitory concentration for human tumor HCT116 cell-line was determined using MTT assay after 3 days of incubation2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Synthesis and antitumor activity of the hexacyclic camptothecin derivatives.
AID1488980Cytotoxicity against human HT-29 cells assessed as growth reduction under hypoxic condition after 72 hrs by MTT assay2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole.
AID248760In vitro inhibitory concentration against human lung large cell carcinoma cell line, H460 (after 1 hour exposure)2004Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
Synthesis and cytotoxic activity of substituted luotonin A derivatives.
AID211091The compound was tested for top1-induced DNA cleavage activity; +++ indicates much more potent than CPT1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Molecular modeling studies of the DNA-topoisomerase I ternary cleavable complex with camptothecin.
AID249965In vitro cytotoxic activity against human SW1783 cancer cell lines after 3 days of culture; Activity expressed as log IC502005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1666197Cytotoxicity against FR-positive human SiHa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging.
AID100463Inhibitory activity in mice bearing L1210 leukemia1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity.
AID1708523Inhibition of human topoisomerase 1 assessed as stabilization of Topl-DNA cleavable complex by measuring DNA cleavage at 50 uM by ethidium bromide dye based agarose gel electrophoresis2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID1703228Solubility of compound in phosphate buffer at pH 4.5 incubated for 24 hrs under shaking condition by HPLC analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID249910In vitro cytotoxic activity against human ACHN cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID150683Tested in vitro for the inhibition of P388 (mouse leukemia) cell line by MTT assay; 1.95-6.93 ng/mL1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues.
AID81341Tested in vitro for the inhibition of HOC-21(human ovarian cancer) cell line by MTT assay1994Journal of medicinal chemistry, Sep-16, Volume: 37, Issue:19
Antitumor agents. 7. Synthesis and antitumor activity of novel hexacyclic camptothecin analogues.
AID680207TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.09uL/oocyte in Xenopus laevis oocytes2004Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity.
AID102138Inhibition against MDA-MB-435 S human breast cancer cells in the presence of 30 mg/mL HSA2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID321559Antiproliferative activity against human MIA PaCa cells after 96 hrs2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
Synthesis and bioevaluation of 22-hydroxyacuminatine analogs.
AID745331Cytotoxicity against mouse L1210 cells2013European journal of medicinal chemistry, May, Volume: 63Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents.
AID249928In vitro cytotoxic activity against human SCC-9 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249926In vitro cytotoxic activity against human Hs 729 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1515332Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID1076084Cytotoxicity against human HCT116 cells assessed as growth inhibition after 3 days by SRB assay2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.
AID681562TP_TRANSPORTER: uptake in BCRP-expressing PC-6 cells2004International journal of cancer, Jul-20, Volume: 110, Issue:6
Novel camptothecin analogues that circumvent ABCG2-associated drug resistance in human tumor cells.
AID1593652Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives.
AID679164TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cell2004Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity.
AID1754551Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs2021Bioorganic & medicinal chemistry letters, 08-15, Volume: 46New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology.
AID249929In vitro cytotoxic activity against human SW948 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID418332Antiproliferative activity against human QG56 cells after 3 days2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Synthesis of new camptothecin analogs with improved antitumor activities.
AID1703227Induction of apoptosis in human HCT-116 cells assessed as early apoptotic cells level at 1 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.17%)2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID1535492Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
Monodisperse oligoethylene glycols modified Camptothecin, 10-Hydroxycamptothecin and SN38 prodrugs.
AID1754552Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth measured after 72 hrs2021Bioorganic & medicinal chemistry letters, 08-15, Volume: 46New camptothecin derivatives for generalized oncological chemotherapy: Synthesis, stereochemistry and biology.
AID1703211Cytotoxicity against human HCT-116 assessed as reduction in cell viability measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID1650404Antiproliferative activity against human G317 cell spheroid assessed as reduction in cell viability incubated for 8 days2020Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1
Pyrazolopyrimide library screening in glioma cells discovers highly potent antiproliferative leads that target the PI3K/mTOR pathway.
AID249938In vitro cytotoxic activity against human Hs 578.T cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID682062TP_TRANSPORTER: uptake in membrane vesicle from PC-6/SN2-5H cells2001Biochemical and biophysical research communications, Nov-09, Volume: 288, Issue:4
Transport of 7-ethyl-10-hydroxycamptothecin (SN-38) by breast cancer resistance protein ABCG2 in human lung cancer cells.
AID1626190Synergistic cytotoxicity in human HT-29 cells assessed as dose reduction index ratio in presence of CoCl2-induced hypoxic conditions measured at 70 % cell growth inhibition after 72 hrs in presence of compound-5c by cell counter method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.
AID1593651Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives.
AID91478Association constant for the binding of the lactone form to human serum albumin;(M aa)e-11994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID222930Association constant for the binding of carboxylate form to human serum albumin1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID249924In vitro cytotoxic activity against human DU145 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249920In vitro cytotoxic activity against human A-498 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249927In vitro cytotoxic activity against human LNCaP cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID28491% lactone at different intervals of time in PBS suspension2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID1666196Cytotoxicity against FR-positive human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2020ACS medicinal chemistry letters, Aug-13, Volume: 11, Issue:8
Folate Receptor Targeting and Cathepsin B-Sensitive Drug Delivery System for Selective Cancer Cell Death and Imaging.
AID680557TP_TRANSPORTER: uptake in OATP1B1-expressing HEK293 cells2004Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity.
AID91476Binding parameter of the lactone form to human serum albumin; n value1994Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1
The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID249966In vitro cytotoxic activity against human CFPAC-1 cancer cell lines after 3 days of culture; Activity expressed as log IC502005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249959In vitro cytotoxic activity against human Detroit 562 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249909In vitro cytotoxic activity against human A549 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1465636AUC (0 to t) in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle.
AID249964In vitro cytotoxic activity against human SW1088 cancer cell lines after 3 days of culture; Activity expressed as log IC502005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID749697Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTS assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1076088Cytotoxicity against human MDA-MB-231 cells2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.
AID1900078Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency
AID411093Cytotoxicity against human HT-29 cells by SRB method2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin.
AID28883Half life of compound in PBS with HSA suspension2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID749701Inhibition of HDAC in human HeLa cells using Fluor-de-Lys as substrate up to 10 uM after 15 mins by fluorescence assay2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID331825Antiproliferative activity against human HT29 cells after 1 hr of drug exposure measured after 72 hrs2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.
AID27448Half-life period in PBS buffer at 37 C in the absence of human serum albumin1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID211111Inhibition of topoisomerase-1 compared to SN-38.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues.
AID249961In vitro cytotoxic activity against human H4 cancer cell lines after 3 days of culture; Activity expressed as log IC502005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1515347Antiproliferative activity against human NCI-H522 cells after 48 hrs by SRB assay2019Bioorganic & medicinal chemistry, 01-15, Volume: 27, Issue:2
Lamellarin-inspired potent topoisomerase I inhibitors with the unprecedented benzo[g][1]benzopyrano[4,3-b]indol-6(13H)-one scaffold.
AID249912In vitro cytotoxic activity against human G361 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249958In vitro cytotoxic activity against human MDA-MB-231 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID249934In vitro cytotoxic activity against human HCT-15 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID682116TP_TRANSPORTER: inhibition of E1S uptake (SN38 10 u M) in OATP1B1-expressing HEK293 cells2004Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity.
AID163139In vitro antitumor activity against QG-56 (human lung cancer) cells.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues.
AID1294918Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by SRB assay2016European journal of medicinal chemistry, Jun-30, Volume: 11610-Boronic acid substituted camptothecin as prodrug of SN-38.
AID249962In vitro cytotoxic activity against human Hs 683 cancer cell lines after 3 days of culture; Activity expressed as log IC502005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1535493Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
Monodisperse oligoethylene glycols modified Camptothecin, 10-Hydroxycamptothecin and SN38 prodrugs.
AID103441Antiproliferative activity against human MCF-7 breast cell line1999Bioorganic & medicinal chemistry letters, Sep-06, Volume: 9, Issue:17
BN 80927: a novel homocamptothecin with inhibitory activities on both topoisomerase I and topoisomerase II.
AID1562006Downregulation of TOP1 expression in human A549 cells at 0.04 uM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID1655975Cytotoxicity against human RPMI7951 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Artemisinin Derivatives with Antimelanoma Activity Show Inhibitory Effect against Human DNA Topoisomerase 1.
AID1294920Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by SRB assay2016European journal of medicinal chemistry, Jun-30, Volume: 11610-Boronic acid substituted camptothecin as prodrug of SN-38.
AID221333In Vitro cytotoxicity against human lung cancer cell line (H128)2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID749695Inhibition of HDAC in human DU145 cells assessed as upregulation of p21waf1 expression at 0.1 to 0.5 uM after 24 hrs by Western blot analysis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID1626188Synergistic cytotoxicity in human HT-29 cells assessed as dose reduction index ratio in presence of CoCl2-induced hypoxic conditions measured at 90 % cell growth inhibition after 72 hrs in presence of compound-5c by cell counter method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.
AID331827Resistant index, ratio of IC50 for BCRP overexpressing mitoxantrone-resistant human HT29 cells to IC50 for human HT29 cells2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.
AID249932In vitro cytotoxic activity against human BxPC-3 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1703224Induction of apoptosis in human HCT-116 cells assessed as late apoptotic cells level at 0.03 uM incubated for 24 hrs by Annexin V-FITC/PI staining based flow cytometry (Rvb = 0.07%)2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID414760Cytotoxicity against BCRP overexpressing human KBH5.0 cells after 4 days by MTT method2009Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7
12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents.
AID1562011Inhibition of topoisomerase 1 in human HCT116 cells assessed as increase in phosphorylated KAP1 expression at 0.04 uM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID1428728Mean residence time in human2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
The long story of camptothecin: From traditional medicine to drugs.
AID102137Inhibition against MDA-MB-435 S human breast cancer cells in the absence of albumin2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID211118Average concentration to cause 50% inhibition of topo 1 using the cleavable complex assay2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1562001Induction of cell cycle arrest in human Capan1 cells at 3 nM after 24 hrs by RNase A/PI-staining based flow cytometric analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID1470600Cytotoxicity against human HT-29 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID1562007Downregulation of TOP1 expression in human HCT116 cells at 0.04 uM after 24 hrs by Western blot analysis2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
AID678799TP_TRANSPORTER: increase of cytotoxicity by GF120918 in T8 cells2001Clinical cancer research : an official journal of the American Association for Cancer Research, Apr, Volume: 7, Issue:4
Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.
AID1703215Cytotoxicity against human Hela assessed as reduction in cell viability measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID1708439Cytotoxicity against wild-type MDCK-II cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site.
AID27126Equilibrium association constant interacting with unilamellar vesicles of negatively charged DMPG in PBS buffer at pH of 7.4 and 37 degrees celsius.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID624634Drug glucuronidation reaction catalyzed by human recombinant UGT1A62005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1900069Solubility of compound in PBS2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
On-Demand Activation of a Bioorthogonal Prodrug of SN-38 with Fast Reaction Kinetics and High Releasing Efficiency
AID624637Drug glucuronidation reaction catalyzed by human recombinant UGT1A92005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID1593646Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives.
AID1470604Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under normoxic condition followed by compound washout measured after 72 hrs by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and biological evaluation of hypoxia-activated prodrugs of SN-38.
AID548078Growth inhibition of human gastric cancer cells after 72 hrs by sulforhodamine B assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and antitumor activity of novel benzimidazole-5-carboxylic acid derivatives and their transition metal complexes as topoisomerease II inhibitors.
AID690587Cytotoxicity against human PC3 cells expressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay2012Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20
Camptothecins in tumor homing via an RGD sequence mimetic.
AID1076085Cytotoxicity against human A549 cells assessed as growth inhibition after 3 days by SRB assay2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.
AID1399552Antiproliferative activity against human A549 cells after 72 hrs by SRB assay2018Bioorganic & medicinal chemistry, 09-01, Volume: 26, Issue:16
A series of camptothecin prodrugs exhibit HDAC inhibition activity.
AID248720In-vitro inhibitory concentration for human tumor BEL-7402 cell-line was determined using MTT assay after 3 days of incubation2005Bioorganic & medicinal chemistry letters, Jul-01, Volume: 15, Issue:13
Synthesis and antitumor activity of the hexacyclic camptothecin derivatives.
AID249913In vitro cytotoxic activity against human HT-29 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1708531Growth inhibition of human LNCaP cells by Cell-titer96 assay2021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID17281Equilibrium association constant interacting with unilamellar vesicles of electroneutral in PBS buffer at pH 7.42000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID222614% of lactone form at equilibrium in human plasma1993Journal of medicinal chemistry, Aug-20, Volume: 36, Issue:17
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
AID1703221Inhibition of colony formation in human HCT-116 cells at 1 nM incubated for 12 days by crystal violet dye based assay2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID249922In vitro cytotoxic activity against human BT-20 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID749698Inhibition of topoisomerase-1 (unknown origin) assessed as reduction of pBR322 plasmid DNA relaxation at 50 uM after 30 mins by agarose gel electrophoresis2013Bioorganic & medicinal chemistry letters, Jun-01, Volume: 23, Issue:11
Dual-acting histone deacetylase-topoisomerase I inhibitors.
AID418334Antiproliferative activity against human PC6 expressing BCRP cells after 6 days2009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Synthesis of new camptothecin analogs with improved antitumor activities.
AID244680Average tumor weight in mouse tumor sarcoma-180 model after intraperitoneal administration of 5 mg/kg dose2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
AID1703212Cytotoxicity against human LoVo assessed as reduction in cell viability measured after 72 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID249915In vitro cytotoxic activity against human PC-3 cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1465631Half life in Beagle dog at 2 mg/kg, iv administered as single bolus dose by LC-MS/MS analysis2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle.
AID418336Inhibition of human topoisomerase 12009Bioorganic & medicinal chemistry letters, Apr-01, Volume: 19, Issue:7
Synthesis of new camptothecin analogs with improved antitumor activities.
AID1167196Intrinsic cytotoxicity against HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay2015Journal of medicinal chemistry, Jan-08, Volume: 58, Issue:1
Converting potent indeno[1,2-b]indole inhibitors of protein kinase CK2 into selective inhibitors of the breast cancer resistance protein ABCG2.
AID1703219Inhibition of human recombinant topoisomerase I using DNA pBR322 as substrate assessed as relaxed DNA at 100 uM incubated for 30 mins by gel electrophoresis analysis relative to control2020European journal of medicinal chemistry, Sep-15, Volume: 202F10, a new camptothecin derivative, was identified as a new orally-bioavailable, potent antitumor agent.
AID1488978Cytotoxicity against human NCI-H460 cells assessed as growth reduction under hypoxic condition after 72 hrs by MTT assay2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole.
AID31609Percent inhibition of acetylcholinesterase using ATCh1 as a substrate2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1488967Drug level in Pd/C using 1 mg 3C-SN38 assessed as compound formation in presence of H2 after 2 hrs by LC/MS method2017ACS medicinal chemistry letters, Jul-13, Volume: 8, Issue:7
Synthesis and Biological Evaluation of Paclitaxel and Camptothecin Prodrugs on the Basis of 2-Nitroimidazole.
AID1708533Inhibition of human topoisomerase 12021Journal of medicinal chemistry, 02-11, Volume: 64, Issue:3
Copper(I)-Catalyzed Nitrile-Addition/
AID331826Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs2008Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9
E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.
AID548080Growth inhibition of human colon cancer cells after 72 hrs by sulforhodamine B assay2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and antitumor activity of novel benzimidazole-5-carboxylic acid derivatives and their transition metal complexes as topoisomerease II inhibitors.
AID1294913Retention time in human MCF7 cells at 10'-5 M by HPLC analysis2016European journal of medicinal chemistry, Jun-30, Volume: 11610-Boronic acid substituted camptothecin as prodrug of SN-38.
AID680549TP_TRANSPORTER: uptake of SN-38 at a concentration of 0.16uL/oocyte in Xenopus laevis oocytes2004Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity.
AID247637Inhibitory concentration against human Bel-7402 liver cancer cell line2005Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8
Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
AID81340In vitro antitumor activity against HOC-21 (human ovarian cancer) cells.1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Synthesis and antitumor activity of ring A- and F-modified hexacyclic camptothecin analogues.
AID28881Half life in human blood.2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID1593648Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by WST8 dye based assay2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis, antibacterial and cytotoxic evaluation of flavipucine and its derivatives.
AID1815776Cytotoxicity against oleic acid-induced human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
The BASHY Platform Enables the Assembly of a Fluorescent Bortezomib-GV1001 Conjugate.
AID249944In vitro cytotoxic activity against human U87MG cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID679166TP_TRANSPORTER: inhibition of Estrone-3-sulfate uptake(Estrone-3-sulfate: 9.2nM) in Xenopus laevis oocytes2004Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 32, Issue:3
Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity.
AID249963In vitro cytotoxic activity against human Hs 766.T cancer cell lines after 3 days of culture; Activity expressed as log IC502005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1182589Inhibition of human recombinant topoisomerase 1 at 100 nM preincubated for 20 mins before addition of supercoiled plasmid DNA by ethidium bromide dye based gel electrophoresis2014Journal of medicinal chemistry, Jul-24, Volume: 57, Issue:14
Design, synthesis, mechanisms of action, and toxicity of novel 20(s)-sulfonylamidine derivatives of camptothecin as potent antitumor agents.
AID219883In Vitro cytotoxicity against human colon cancer cell line (WiDr)2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID216616Percentage of 50% or greater regression (PR) against WiDr xenografts in nude mice at a dose of 10 umol/kg2001Journal of medicinal chemistry, May-10, Volume: 44, Issue:10
Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1194767Cytotoxicity against human HCT116 cells after 72 hrs by sulforhodamine B assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design, synthesis and biological evaluation of novel homocamptothecin analogues as potent antitumor agents.
AID28492% lactone at different intervals of time in PBS with HSA suspension2000Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21
The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID249930In vitro cytotoxic activity against human T-47D cancer cell lines after 3 days of culture2005Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3
Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347169Tertiary RLuc qRT-PCR qHTS assay for Zika virus inhibitors2020Proceedings 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.
AID1347411qHTS 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) Libary2020ACS 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.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS 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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
AID1347161Confirmatory screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347157Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS2020Proceedings 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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings 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]

Research

Studies (85)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (9.41)18.2507
2000's32 (37.65)29.6817
2010's28 (32.94)24.3611
2020's17 (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: 56.14

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.

MetricThis Compound (vs All)
Research Demand Index56.14 (24.57)
Research Supply Index4.47 (2.92)
Research Growth Index4.93 (4.65)
Search Engine Demand Index88.88 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (56.14)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.18%)5.53%
Reviews4 (4.71%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other80 (94.12%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]