FSL0608
- Structure
- InChI=1S/C20H24N2O2S/c1-3-22(4-2)12-11-21-16-10-9-14(13-23)20-18(16)19(24)15-7-5-6-8-17(15)25-20/h5-10,21,23H,3-4,11-13H2,1-2H3
- InChIKey=MFZWMTSUNYWVBU-UHFFFAOYSA-N
- Synonyms
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- Origin
- Chemically synthesized
- Biological activities
- Inhibition of DNA repair
- Therapeutic
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Anticancer
Antischistosomiasis
- Target
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Apurinic endonuclease-1 (APE1)
- Assay information
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Schistosomicidal activity for experimentary schistosoma infected hamsters (ED50: 0.78 mg/kg, per os)
Antitumor activity for P388 lymphocytic leukemia-bearing mice
Inhibition of APE1 endonuclease activity by direct binding to the hydrophobic site (Kd = 10 nM)
- References
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Naidu MD, Agarwal R, Pena LA, Cunha L, Mezei M, Shen M, Wilson DM 3rd, Liu Y, Sanchez Z, Chaudhary P, Wilson SH, Waring MJ
Lucanthone and its derivative hycanthone inhibit apurinic endonuclease-1 (APE1) by direct protein binding.
PLoS One, 6(9): e23679 (2011) 21935361 doi: 10.1371/journal.pone.0023679
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Archer S, Pica-Mattoccia L, Cioli D, Seyed-Mozaffari A, Zayed AH
Preparation and antischistosomal and antitumor activity of hycanthone and some of its congeners. Evidence for the mode of action of hycanthone.
J Med Chem, 31(1): 254-260 (1988) 3336024
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Rosi D, Peruzzotti G, Dennis EW, Berberian DA, Freele H, Archer S
A new active metabolite of "Miracil D".
Nature, 208(5014): 1005-1006 (1965) 4958061