FSL0803
- Structure
- InChI=1S/C22H22O8/c1-25-16-4-10(5-17(26-2)21(16)27-3)18-11-6-14-15(30-9-29-14)7-12(11)20(23)13-8-28-22(24)19(13)18/h4-7,13,18-20,23H,8-9H2,1-3H3/t13-,18+,19-,20-/m0/s1
- InChIKey=YJGVMLPVUAXIQN-XVVDYKMHSA-N
- Synonyms
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- 518-28-5
- podofilox
- Podophyllotoxin
- Origin
- Podophyllum peltatum
- Biological activities
- antineoplastic
Inhibition of tubulin polymerization
- Therapeutic
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Anticancer
- Target
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Tubulin
Topoisomerase II
- Assay information
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Treat of SV40 virusinfected BSC cells at various times postinfection by VM-26, podophyllotoxin derivertive (100 μM, 20 min)
Accumulation of metaphase (Kmet) for total of 50% of the cells (approximately 30 nM, peak of maximal metaphase accumulation = 100 nM)
Decrease of the ratio of cells in anaphase to cells by metaphase in a concentration-dependent manner, (50% decrease = 5 nM (Kana/met))
Zero of the anaphase/metaphase ratio (33 nM). Half-maximal inhibition of cell division (Kdiv) (IC50 = 20 nM)
Model compound in structure-activity relationship study because of a large number of semisynthetic derivatives
- References
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Naik PK, Alam A, Malhotra A, Rizvi O
Molecular modeling and structure-activity relationship of podophyllotoxin and its congeners.
J Biomol Screen, 15(5): 528-540 (2010) 20460251 doi: 10.1177/1087057110368994
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Canel C, Moraes RM, Dayan FE, Ferreira D
Podophyllotoxin.
Phytochemistry, 54(2): 115-120 (2000) 10872202
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Jordan MA, Thrower D, Wilson L
Effects of vinblastine, podophyllotoxin and nocodazole on mitotic spindles. Implications for the role of microtubule dynamics in mitosis.
J Cell Sci, 102 ( Pt 3): 401-416 (1992) 1506423
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Yang L, Rowe TC, Liu LF
Identification of DNA topoisomerase II as an intracellular target of antitumor epipodophyllotoxins in simian virus 40-infected monkey cells.
Cancer Res, 45(11 Pt 2): 5872-5876 (1985) 2996763
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Ross W, Rowe T, Glisson B, Yalowich J, Liu L
Role of topoisomerase II in mediating epipodophyllotoxin-induced DNA cleavage.
Cancer Res, 44(12 Pt 1): 5857-5860 (1984) 6094001