Compounds > 3-tritylthio-l-alanine
Page last updated: 2024-12-07

3-tritylthio-l-alanine

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

Cross-References

ID SourceID
PubMed CID76044
CHEMBL ID392695
CHEBI ID91461
SCHEMBL ID768203
MeSH IDM0044817

Synonyms (48)

Synonym
l-cysteine, s-(triphenylmethyl)-,
brn 2339626
nsc 124663
s-(triphenylmethyl)-l-cysteine
NCIMECH_000214
nsc 83265
s-trityl-l-cysteine
2799-07-7
alanine, 3-(tritylthio)-, l-
s-tritylcysteine
(+)-s-trityl-l-cysteine, 97%
stlc
chembl392695 ,
s-trityl-l-cysteine (stlc), 1
(2r)-2-amino-3-[(triphenylmethyl)sulfanyl]propanoic acid
bdbm23772
h-cys(trt)-oh
T2522
zzd ,
EN300-72024
A819272
(r)-2-amino-3-tritylsulfanyl-propionic acid
CCG-35305
4-06-00-05051 (beilstein handbook reference)
AKOS015897303
AKOS015854129
S5522
2(r)-amino-3-tritylsulfanylpropionic acid
(r)-2-amino-3-(tritylthio)propanoic acid
MLS006010852
smr004701775
AM81687
SCHEMBL768203
J-300091
(+)-s-trityl-l-cysteine
CHEBI:91461
CS-W011818
Q27163302
(2r)-2-amino-3-[(triphenylmethyl)thio]propanoic acid
AS-11885
cysteine(trt)-oh
trityl-l-cysteine
M03084
s-trityl-cysteine
HY-W011102
d-cysteine,s-(triphenylmethyl)-
Z1143441519
(2r)-2-amino-3-[tri(phenyl)methylsulfanyl]propanoic acid

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" One triphenylbutanamine analogue and ispinesib possess very good bioavailability (51% and 45%, respectively), with the former showing in vivo antitumor growth activity in nude mice xenograft studies."( Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
Good, JA; Kaan, HY; Kozielski, F; Mackay, SP; Rath, O; Sutcliffe, OB; Wang, F, 2012)		0.38
" They have good oral bioavailability and pharmacokinetics and induced complete tumor regression in nude mice explanted with lung cancer patient xenografts."( Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
Good, JA; Kaan, HY; Kozielski, F; MacKay, SP; Podgórski, D; Rath, O; Talapatra, SK; Wang, F, 2013)		0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzenoid aromatic compound
[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]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Delta-type opioid receptorMus musculus (house mouse)Ki0.02600.00000.53939.4000AID320366
Kinesin-like protein KIF11Homo sapiens (human)IC50 (µMol)0.82270.00011.405710.0000AID1255273; AID1353895; AID1800334; AID299460; AID320367; AID320369; AID586585; AID614342; AID667248; AID740549; AID740550; AID765745
Kinesin-like protein KIF11Homo sapiens (human)Ki0.08920.00050.06310.1438AID1798360; AID320366; AID320370; AID586584; AID659273; AID659274; AID725983; AID728344
[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)
Kinesin-like protein KIF11Homo sapiens (human)EC50 (µMol)1.72001.72001.72001.7200AID614343
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
mitotic cell cycleKinesin-like protein KIF11Homo sapiens (human)
microtubule-based movementKinesin-like protein KIF11Homo sapiens (human)
spindle organizationKinesin-like protein KIF11Homo sapiens (human)
mitotic spindle organizationKinesin-like protein KIF11Homo sapiens (human)
mitotic centrosome separationKinesin-like protein KIF11Homo sapiens (human)
regulation of mitotic centrosome separationKinesin-like protein KIF11Homo sapiens (human)
cell divisionKinesin-like protein KIF11Homo sapiens (human)
mitotic spindle assemblyKinesin-like protein KIF11Homo sapiens (human)
spindle elongationKinesin-like protein KIF11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
microtubule motor activityKinesin-like protein KIF11Homo sapiens (human)
protein bindingKinesin-like protein KIF11Homo sapiens (human)
ATP bindingKinesin-like protein KIF11Homo sapiens (human)
microtubule bindingKinesin-like protein KIF11Homo sapiens (human)
protein kinase bindingKinesin-like protein KIF11Homo sapiens (human)
plus-end-directed microtubule motor activityKinesin-like protein KIF11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
spindle poleKinesin-like protein KIF11Homo sapiens (human)
spindle microtubuleKinesin-like protein KIF11Homo sapiens (human)
spindleKinesin-like protein KIF11Homo sapiens (human)
cytosolKinesin-like protein KIF11Homo sapiens (human)
microtubuleKinesin-like protein KIF11Homo sapiens (human)
membraneKinesin-like protein KIF11Homo sapiens (human)
mitotic spindleKinesin-like protein KIF11Homo sapiens (human)
kinesin complexKinesin-like protein KIF11Homo sapiens (human)
protein-containing complexKinesin-like protein KIF11Homo sapiens (human)
nucleusKinesin-like protein KIF11Homo sapiens (human)
mitotic spindleKinesin-like protein KIF11Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (119)

Assay IDTitleYearJournalArticle
AID659273Inhibition of N-terminal hexa-histidine tagged human cloned Eg5 (1 to 368 amino acids) expressed in Escherichia coli BL21 (DE3) assessed as reduction in basal ATPase activity by pyruvate kinase/lactate dehydrogenase-linked assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
AID614396Growth inhibition of human SW620 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID725983Inhibition of MT-stimulated human N-terminal His6-tagged Eg5 (1 to 368 amino acid residues) motor domain ATPase activity expressed in Escherichia coli BL21 (DE3) by pyruvate kinase/lactate dehydrogenase-coupled assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
AID614412Growth inhibition of human OVCAR3 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614353Growth inhibition of human CCRF-CEM cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614359Growth inhibition of human A549 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID320372Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 1 uM after 24 hrs2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID614403Growth inhibition of human LOXIMVI cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID659271Antiproliferative activity against human K562 cells after 72 hrs by Alamar blue assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
AID586594Growth inhibition of pig L-MDR1 cells overexpressing human P-glycoprotein in presence of P-glycoprotein inhibitor LY3359792011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID586587Growth inhibition of dog MDCK2-MDR1 cells overexpressing human P-glycoprotein2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID614420Growth inhibition of human SN12C cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID1353895Inhibition of mitotic kinesin Eg5 (unknown origin)2018European journal of medicinal chemistry, Mar-25, Volume: 148Synthesis of N-(1-(6-acetamido-5-phenylpyrimidin-4-yl) piperidin-3-yl) amide derivatives as potential inhibitors for mitotic kinesin spindle protein.
AID586584Inhibition of C-terminal His6-tagged human Eg5 basal ATPase activity2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID320367Inhibition of microtubule-activated Eg5 ATPase activity2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID586590Ratio of GI50 for dog MDCK2-MDR1 cells overexpressing human P-glycoprotein to GI50 for dog MDCK2 cells2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID299462Cell cycle arrest in HeLa cells assessed as 50 percent arrest at M phase after 20 hrs2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
AID320375Induction of mitotic arrest in human HeLa cells at 5 uM assessed as MPM2 antibody positive cells after 24 hrs2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID1255273Inhibition of His-tagged KSP motor domain (1 to 369) (unknown origin) assessed as inhibition of microtubule-stimulated KSP ATPase activity preincuabted for 30 mins followed by ATP addition measured after 15 mins by Kinase-Glo assay2015ACS medicinal chemistry letters, Sep-10, Volume: 6, Issue:9
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors.
AID614418Growth inhibition of human ACHN cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614405Growth inhibition of human M14 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614369Growth inhibition of human HCT15 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID659274Inhibition of N-terminal hexa-histidine tagged human cloned Eg5 (1 to 368 amino acids) expressed in Escherichia coli BL21 (DE3) assessed as reduction of MT-stimulated ATPase activity by pyruvate kinase/lactate dehydrogenase-linked assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
AID740549Inhibition of human Eg5 catalytic domain basal ATPase activity after 25 mins by spectrophotometric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.
AID320368Growth inhibition of human NCI60 cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID1255274Growth inhibition of human HCT116 cells after 72 hrs by MTS assay2015ACS medicinal chemistry letters, Sep-10, Volume: 6, Issue:9
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors.
AID320370Inhibition of human Eg5 basal ATPase activity2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID644332Inhibition of HCV genotype 1b recombinant N-His-tagged NS5B Cdelta21 polymerase expressed in Escherichia coli DH5alpha using [alpha-32P]UTP at 100 uM after 60 mins by liquid scintillation counting2012European journal of medicinal chemistry, Mar, Volume: 49Inhibition of hepatitis C virus NS5B polymerase by S-trityl-L-cysteine derivatives.
AID659432Antiproliferative activity against human NCI-H1299 cells after 72 hrs by Alamar blue assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
AID726023Growth inhibition of human LNCAP cells after 72 hrs by Alamar blue assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
AID614404Growth inhibition of human MALME-3M cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614422Growth inhibition of human UO31 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614397Growth inhibition of human SF268 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614357Growth inhibition of human RPMI8266 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614360Growth inhibition of human EKVX cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID667247Binding affinity to mitotic kinesin Eg5 by isothermal colorimetric assay2012European journal of medicinal chemistry, Aug, Volume: 54Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.
AID614356Growth inhibition of human MOLT4 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614363Growth inhibition of human NCI-H23 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID659433Antiproliferative activity against human BxPC3 cells after 72 hrs by Alamar blue assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
AID728342Growth inhibition of human K562 cells after 72 hrs by Alamar blue assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
AID614414Growth inhibition of human OVCAR5 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID765743Inhibition of microtubule-stimulated ATPase activity of human Eg5 D130V mutant expressed in Escherichia coli BL21 by pyruvate kinase/lactate dehydrogenase-linked assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism.
AID586585Inhibition of C-terminal His6-tagged human Eg5 microtubule-stimulated ATPase activity2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID614368Growth inhibition of human HCT116 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID1611277Induction of cell cycle arrest in human HeLa cells assessed as mono-polar spindles formation surrounded by ring shaped chromosomes in mitotic cells at 3 uM incubated for 6 hrs by Hoechst 33342 staining based confocal microscopic method2019Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
Pyrenocine A induces monopolar spindle formation and suppresses proliferation of cancer cells.
AID726021Growth inhibition of human BxPC3 cells after 72 hrs by Alamar blue assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
AID659430Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
AID299463Inhibition of CENPE assessed as inhibition ATP hydrolysis by ATPase assay at 20 uM2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
AID614365Growth inhibition of human NCI-H522 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID586592Growth inhibition of pig L-MDR1 cells overexpressing human P-glycoprotein2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID320373Cell cycle arrest in human HeLa cells assessed as accumulation at G2/M phase at 5 uM after 24 hrs2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID740790Antiproliferative activity against human NCI60 cells2013European journal of medicinal chemistry, Apr, Volume: 62Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.
AID586591Growth inhibition of pig LLC-PK1 cells2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID586583Induction of mitotic arrest in human HeLa cells2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID614398Growth inhibition of human SF295 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614417Growth inhibition of human 786-0 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614409Growth inhibition of human UACC257 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID667248Inhibition of basal ATPase activity of Eg5 by coupled pyruvate kinase/lactate dehydrogenase assay2012European journal of medicinal chemistry, Aug, Volume: 54Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.
AID740550Inhibition of human Eg5 catalytic domain assessed as inhibition of microtubulin-induced ATPase activity after 25 mins by spectrophotometric analysis2013European journal of medicinal chemistry, Apr, Volume: 62Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.
AID667251Cytotoxicity against human NCI-H1299 cells after 72 hrs by Alamar blue assay2012European journal of medicinal chemistry, Aug, Volume: 54Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.
AID614355Growth inhibition of human K562 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614408Growth inhibition of human SK-MEL-5 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID299464Inhibition of Kid assessed as inhibition ATP hydrolysis by ATPase assay at 20 uM2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
AID614411Growth inhibition of human IGROV1 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID299465Inhibition of MKLP1 assessed as inhibition ATP hydrolysis by ATPase assay at 20 uM2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
AID614358Growth inhibition of human SR cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID586586Growth inhibition of dog MDCK2 cells2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID614419Growth inhibition of human Caki1 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614366Growth inhibition of human COLO205 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614351Inhibition of Drosophila melanogaster Klp61F in S2 cells at 100 uM up to 7 hrs by immunofluorescence analysis2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614415Growth inhibition of human OVCAR8 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614402Growth inhibition of human U251 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID1611279Inhibition of human Eg5 motor domain (1 to 368 residues) expressed in Escherichia coli assessed as reduction in microtubule-stimulated ATPase activity at 3 uM incubated with ATP for 6 mins by malachite green method2019Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
Pyrenocine A induces monopolar spindle formation and suppresses proliferation of cancer cells.
AID614362Growth inhibition of human NCI-H226 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID644333Inhibition of HCV genotype 1b recombinant N-His-tagged NS5B Cdelta21 polymerase expressed in Escherichia coli DH5alpha using [alpha-32P]UTP after 60 mins by liquid scintillation counting2012European journal of medicinal chemistry, Mar, Volume: 49Inhibition of hepatitis C virus NS5B polymerase by S-trityl-L-cysteine derivatives.
AID586595Ratio of GI50 for pig L-MDR1 cells overexpressing human P-glycoprotein to GI50 for pig LLC-PK1 cells2011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID614399Growth inhibition of human SF539 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614400Growth inhibition of human SNB19 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID667252Cytotoxicity against human BxPC3 cells after 72 hrs by Alamar blue assay2012European journal of medicinal chemistry, Aug, Volume: 54Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.
AID1150970Antitumor activity against mouse TA3 cells assessed as growth inhibition1976Journal of medicinal chemistry, Aug, Volume: 19, Issue:8
Cysteine derivatives with reactive groups as potential antitumor agents.
AID667249Cytotoxicity against human K562 cells after 72 hrs by Alamar blue assay2012European journal of medicinal chemistry, Aug, Volume: 54Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.
AID586593Growth inhibition of pig LLC-PK1 cells in presence of P-glycoprotein inhibitor LY3359792011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID614395Growth inhibition of human KM12 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614416Growth inhibition of human SKOV3 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID728344Inhibition of human N-terminal His6-tagged Eg5 (1 to 368 amino acid residues) motor domain basal ATPase activity expressed in Escherichia coli BL21 (DE3) by pyruvate kinase/lactate dehydrogenase-coupled assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
AID765745Inhibition of microtubule-stimulated ATPase activity of N-terminal His-6-tagged human wild type Eg5 (1 to 368) expressed in Escherichia coli BL21 by pyruvate kinase/lactate dehydrogenase-linked assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism.
AID614342Inhibition of human recombinant microtubule-activated KSP motor domain ATPase activity after 10 mins by end-point assay2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID586589Growth inhibition of dog MDCK2-MDR1 cells overexpressing human P-glycoprotein in presence of P-glycoprotein inhibitor LY3359792011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID614352Inhibition of bipolar spindle formation in Strongylocentrotus purpuratus eggs2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614361Growth inhibition of human HOP62 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614343Inhibition of KSP in human HeLa cells assessed as bipolar spindle formation2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID726024Growth inhibition of human PC3 cells after 72 hrs by Alamar blue assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
AID614354Growth inhibition of human HL-60(TB) cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID728336Growth inhibition of human HCT116 cells after 72 hrs by Alamar blue assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
AID614367Growth inhibition of human HCC2998 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID1255275Binding affinity to KSP motor domain (unknown origin) assessed as change in melting temperature at 100 uM by differential scanning fluorimetry in presence of 1 mM ATP2015ACS medicinal chemistry letters, Sep-10, Volume: 6, Issue:9
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors.
AID614413Growth inhibition of human OVCAR4 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614401Growth inhibition of human SNB75 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614410Growth inhibition of human UACC62 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID320371Induction of mitotic arrest in human HeLa cells assessed as monoastral spindle formation after 24 hrs2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID320366Inhibition of Eg5 ATPase activity2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID765744Inhibition of microtubule-stimulated ATPase activity of human Eg5 A133D mutant expressed in Escherichia coli BL21 by pyruvate kinase/lactate dehydrogenase-linked assay2013Journal of medicinal chemistry, Aug-22, Volume: 56, Issue:16
Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism.
AID614407Growth inhibition of human SK-MEL-28 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID320374Induction of mitotic arrest in human HeLa cells after 24 hrs2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID299460Inhibition of Eg5 assessed as inhibition ATP hydrolysis by ATPase assay2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
AID299461Cytotoxic activity against HeLa cells2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
AID726022Growth inhibition of human NCI-H1299 cells after 72 hrs by Alamar blue assay2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
AID299466Inhibition of KIF4 assessed as inhibition ATP hydrolysis by ATPase assay at 20 uM2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
AID659431Antiproliferative activity against human hTERT-HME1 cells after 72 hrs by Alamar blue assay2012Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
AID614394Growth inhibition of human HT-29 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614406Growth inhibition of human SK-MEL-2 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614364Growth inhibition of human NCI-H322M cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID320369Inhibition of Eg5 assessed as effect on microtubule gliding by cell based motility assay2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID614349Induction of KSP depletion in human HeLa cells after 4 hrs by immunofluorescence analysis2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID614421Growth inhibition of human TK10 cells2011Bioorganic & medicinal chemistry, Sep-15, Volume: 19, Issue:18
Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity.
AID667250Cytotoxicity against human HCT116 cells after 72 hrs by Alamar blue assay2012European journal of medicinal chemistry, Aug, Volume: 54Doing the methylene shuffle--further insights into the inhibition of mitotic kinesin Eg5 with S-trityl L-cysteine.
AID586588Growth inhibition of dog MDCK2 cells in presence of P-glycoprotein inhibitor LY3359792011Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6
Structure-activity relationship and multidrug resistance study of new S-trityl-L-cysteine derivatives as inhibitors of Eg5.
AID1798360Inhibition of Eg5 ATPase Activity from Article 10.1021/jm070606z: \\Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.\\2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Structure-activity relationship of S-trityl-L-cysteine analogues as inhibitors of the human mitotic kinesin Eg5.
AID1800334Microtubule-activated ATPase Kinetic Assay from Article 10.1002/cbic.201402089: \\Structure-based design of new KSP-Eg5 inhibitors assisted by a targeted multicomponent reaction.\\2014Chembiochem : a European journal of chemical biology, Jul-07, Volume: 15, Issue:10
Structure-based design of new KSP-Eg5 inhibitors assisted by a targeted multicomponent reaction.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (6.67)18.7374
1990's0 (0.00)18.2507
2000's2 (13.33)29.6817
2010's12 (80.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.42

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.42 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index5.25 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (6.67%)5.53%
Reviews1 (6.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (86.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gossypol
Gossypol: A dimeric sesquiterpene found in cottonseed (GOSSYPIUM). The (-) isomer is active as a male contraceptive (CONTRACEPTIVE AGENTS, MALE) whereas toxic symptoms are associated with the (+) isomer.		3.1810
cysteine
[no description available]		2.0310cysteine zwitterion;
cysteine;
L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid		EC 4.3.1.3 (histidine ammonia-lyase) inhibitor;
flour treatment agent;
human metabolite
vincristine
[no description available]		2.0610acetate ester;
formamides;
methyl ester;
organic heteropentacyclic compound;
organic heterotetracyclic compound;
tertiary alcohol;
tertiary amino compound;
vinca alkaloid		antineoplastic agent;
drug;
microtubule-destabilising agent;
plant metabolite;
tubulin modulator
trityl chloride
[no description available]		2.0410
s-methylcysteine
S-methylcysteine: RN given refers to parent cpd without isomeric designation. S-methylcysteine : A cysteine derivative that is L-cysteine in which the hydrogen attached to the sulfur is replaced by a methyl group.		2.0310S-alkyl-L-cysteine zwitterion;
S-alkyl-L-cysteine		human urinary metabolite;
plant metabolite
s-2-aminoethyl cysteine
S-2-aminoethyl cysteine: inhibits protein synthesis in mammalian cells; RN given refers to parent cpd; structure. L-thialysine : A cysteine derivative that is the S-(2-aminoethyl) analogue of L-cysteine; reported to have cytotoxic effects.		2.0310L-cysteine thioether;
non-proteinogenic L-alpha-amino acid		EC 5.4.3.2 (lysine 2,3-aminomutase) inhibitor;
metabolite;
protein synthesis inhibitor
s-benzylcysteine
[no description available]		2.0310S-aryl-L-cysteine zwitterion
carbocysteine
Carbocysteine: A compound formed when iodoacetic acid reacts with sulfhydryl groups in proteins. It has been used as an anti-infective nasal spray with mucolytic and expectorant action.. S-carboxymethyl-L-cysteine : An L-cysteine thioether that is L-cysteine in which the hydrogen of the thiol group has been replaced by a carboxymethyl group.		2.0310L-cysteine thioether;
non-proteinogenic L-alpha-amino acid		mucolytic
(S)-monastrol
[no description available]		2.0610ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate
k 858
K 858: an Eg5 inhibitor and antineoplastic agent; structure in first source		3.1810benzenes
monastrol
monastrol: stops mitosis by fostering formation of monopolar spindles; structure in first source. (S)-monastrol : An ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate that has S configuration.. monastrol : A racemate comprising equimolar amounts of R- and S-monastrol.. ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate : A member of the class of thioureas that is 3,4-dihydropyrimidine-2(1)-thione substituted by a 3-hydroxyphenyl group at position 4, an ethoxycarbonyl group at position 5, and a methyl group at position 6.		3.5820enoate ester;
ethyl ester;
phenols;
racemate;
thioureas		antileishmanial agent;
antimitotic;
antineoplastic agent;
EC 3.5.1.5 (urease) inhibitor
wedelolactone
wedelolactone: antihepatotoxic coumestan from Eclipta prostrata and Wedelia calendulacea (both Asteraceae); structure given in first source. wedelolactone : A member of the class of coumestans that is coumestan with hydroxy substituents as positions 1, 8 and 9 and a methoxy substituent at position 3.		2.0710aromatic ether;
coumestans;
delta-lactone;
polyphenol		antineoplastic agent;
apoptosis inducer;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
hepatoprotective agent;
metabolite
ispinesib
[no description available]		2.7830benzamides
3-tritylthio-l-alanine, (d)-isomer
[no description available]		2.4720
sb 743921
[no description available]		5.2631
adociasulfate-2
adociasulfate-2: inhibits kinesin ATPase; from marine sponge Haliclona (also known as Adocia) sp.; structure in first source		3.1810
terpendole e
terpendole E: structure in first source		3.1810organic heterotricyclic compound;
organooxygen compound
arry 520
filanesib: a kinesin spindle protein inhibitor		3.620
ConditionIndicatedRelationship StrengthStudiesTrials
Adenocarcinoma, Basal Cell
[description not available]		01.9510
Experimental Mammary Neoplasms
[description not available]		01.9510
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		01.9510
Hepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted
[description not available]		02.0710
Hepatitis C
INFLAMMATION of the LIVER in humans caused by HEPATITIS C VIRUS, a single-stranded RNA virus. Its incubation period is 30-90 days. Hepatitis C is transmitted primarily by contaminated blood parenterally and is often associated with transfusion and intravenous drug abuse. However, in a significant number of cases, the source of hepatitis C infection is unknown.		02.0710
Cancer of Lung
[description not available]		02.0810
Lung Neoplasms
Tumors or cancer of the LUNG.		02.0810
Benign Neoplasms
[description not available]		03.7330
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		03.7330