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Literature summary for 5.6.2.2 extracted from

  • Cho, H.J.; Jung, M.J.; Kwon, Y.; Na, Y.
    Oxiranylmethyloxy or thiiranylmethyloxy-azaxanthones and -acridone analogues as potential topoisomerase I inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 6766-6769.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-ethyl-3-(benzimidazol-2-yl)-6,8-difluoro-7-(3-methylpiperazin-1-yl)-4(1H)-quinolone 18% and 13% inhibition at 0.1 mM and 0.02 mM, respectively Homo sapiens
1-ethyl-3-(benzimidazol-2-yl)-6-fluoro-7-(1-piperazin-1-yl)-1,8-naphthyridine-4(1H)-one 8% and 30% inhibition at 0.02 mM and 0.1 mM, respectively Homo sapiens
1-ethyl-3-(benzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone 8.5% and 7% inhibition at 0.02 mM and 0.1 mM, respectively Homo sapiens
3-thiiranylmethyloxy-1-hydroxy-5-azaxanthone 19.5% and 9% inhibition at 0.1 mM and 0.02 mM, respectively Homo sapiens
6,8-bis(oxiran-2-ylmethoxy)benzo[b][1,8]naphthyridin-5(10H)-one 9% and 13% inhibition at 0.02 mM and 0.1 mM, respectively Homo sapiens
6,8-bis(thiiran-2-ylmethoxy)benzo[b][1,8]naphthyridin-5(10H)-one 8.5% and 7% inhibition at 0.02 mM and 0.1 mM, respectively Homo sapiens
6-hydroxy-8-(thiiran-2-ylmethoxy)benzo[b][1,8]naphthyridin-5(10H)-one 8% and 9% inhibition at 0.02 mM and 0.1 mM, respectively Homo sapiens
adriamycin
-
Homo sapiens
camptothecin
-
Homo sapiens
etoposide
-
Homo sapiens
additional information inhibitory and cytotoxic potencies of inhibitor compounds, in vivo activity in cancer cell lines, overview. No or poor inhibition by compounds 6, 7, 9, 10, and 11 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
nucleus
-
Homo sapiens 5634
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell
-
Homo sapiens
-
HeLa cell
-
Homo sapiens
-
HL-60 cell
-
Homo sapiens
-
HT-29 cell
-
Homo sapiens
-
MDA-MB-231 cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
Topoisomerase II
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
inhibitor IC50 values in vivo in different cancer cell lines, overview Homo sapiens additional information