FSL0551
- Structure
- InChI=1S/C29H32O13/c1-11-36-9-20-27(40-11)24(31)25(32)29(41-20)42-26-14-7-17-16(38-10-39-17)6-13(14)21(22-15(26)8-37-28(22)33)12-4-18(34-2)23(30)19(5-12)35-3/h4-7,11,15,20-22,24-27,29-32H,8-10H2,1-3H3/t11?,15?,20-,21-,22+,24-,25-,26?,27-,29?/m1/s1
- InChIKey=VJJPUSNTGOMMGY-GEGAHKOSSA-N
- Synonyms
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- Origin
- Chemically synthesized
- Biological activities
- antineoplastic
Induction of DNA damage
- Therapeutic
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Anticancer
- Target
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Topoisomerase II (TOP-2)
- Assay information
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Inhibition of TOP-2 activity (MIC = 0.1 μM)
Induction for accumulation of Phosphorylated histone H2AX, a hallmark of DNA double- strand breaks in cells, in HeLa cells (10 μM)
Induction of apoptosis in cancer cells: HL-60, U937 and A549 (IC50: 0.25 ± 0.04, 0.92 ± 0.24 and 5.9 ± 1.7 μM)
Induction of DNA cleavage complex formation due to the interaction with D-ring of etoposide
Treating fibrosarma in tumor-bearing mice using etoposide entrapped camel milk phospholipids liposomes
- References
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Maswadeh HM, Aljarbou AN, Alorainy MS, Alsharidah MS, Khan MA
Etoposide incorporated into camel milk phospholipids liposomes shows increased activity against fibrosarcoma in a mouse model.
Biomed Res Int, 2015: 743051 (2015) 25821817 doi: 10.1155/2015/743051
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Pitts SL, Jablonksy MJ, Duca M, Dauzonne D, Monneret C, Arimondo PB, Anklin C, Graves DE, Osheroff N
Contributions of the D-Ring to the activity of etoposide against human topoisomerase IIα: potential interactions with DNA in the ternary enzyme--drug--DNA complex.
Biochemistry, 50(22): 5058-5066 (2011) 21548574 doi: 10.1021/bi200531q
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Triana J, Eiroa JL, Ortega JJ, León F, Brouard I, Torres F, Quintana J, Estévez F, Bermejo J
Sesquiterpene lactones from Gonospermum gomerae and G. fruticosum and their cytotoxic activities.
J Nat Prod, 71(12): 2015-2020 (2008) 19053514 doi: 10.1021/np800474v
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Martins LM, Mesner PW, Kottke TJ, Basi GS, Sinha S, Tung JS, Svingen PA, Madden BJ, Takahashi A, McCormick DJ, Earnshaw WC, Kaufmann SH
Comparison of caspase activation and subcellular localization in HL-60 and K562 cells undergoing etoposide-induced apoptosis.
Blood, 90(11): 4283-4296 (1997) 9373239
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Burden DA, Kingma PS, Froelich-Ammon SJ, Bjornsti MA, Patchan MW, Thompson RB, Osheroff N
Topoisomerase II.etoposide interactions direct the formation of drug-induced enzyme-DNA cleavage complexes.
J Biol Chem, 271(46): 29238-29244 (1996) 8910583
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Janin YL, Croisy A, Riou JF, Bisagni E
Synthesis and evaluation of new 6-amino-substituted benzo[c]phenanthridine derivatives.
J Med Chem, 36(23): 3686-3692 (1993) 8246238
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Keller-Juslén C, Kuhn M, Stähelin H, von Wartburg A
Synthesis and antimitotic activity of glycosidic lignan derivatives related to podophyllotoxin.
J Med Chem, 14(10): 936-940 (1971) 5165570