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Literature summary for 5.6.2.1 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 9% and 11% inhibition at 0.1 mM and 0.02 mM, respectively Homo sapiens
3-thiiranylmethyloxy-1-hydroxy-5-azaxanthone 50% and 27% inhibition at 0.1 mM and 0.02 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 1-ethyl-3-(benzimidazol-2-yl)-6-fluoro-7-(piperazin-1-yl)-4(1H)-quinolone, 1-ethyl-3-(benzimidazol-2-yl)-6-fluoro-7-(1-piperazin-1-yl)-1,8-naphthyridine-4(1H)-one, 6,8-bis(oxiran-2-ylmethoxy)benzo[b][1,8]naphthyridin-5(10H)-one, 6-hydroxy-8-(thiiran-2-ylmethoxy)benzo[b][1,8]naphthyridin-5(10H)-one, and 8-bis(thiiran-2-ylmethoxy)benzo[b][1,8]naphthyridin-5(10H)-one 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 I
-
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