The synthesis and the in vitro cytotoxicity studies of bisnaphthalimidopropyl polyamine derivatives against colon cancer cells and parasite Leishmania infantum

Bisnaphthalimidopropyl derivatives (BNIPSpd, BNIPDaoct, BNIPDanon, BNIPDadec, BNIPDpta and BNIPDeta) were synthesised in yields ranging from 50% to 70% and their cytotoxicity against colon cancer cells (Caco-2) and the parasite Leishmania infantum determined using the MTT assay. Cytotoxicity within...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2007, Vol.15 (1), p.541-545
Hauptverfasser: Oliveira, João, Ralton, Lynda, Tavares, Joana, Codeiro-da-Silva, Anabela, Bestwick, Charles S., McPherson, Anne, Thoo Lin, Paul Kong
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Sprache:eng
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Zusammenfassung:Bisnaphthalimidopropyl derivatives (BNIPSpd, BNIPDaoct, BNIPDanon, BNIPDadec, BNIPDpta and BNIPDeta) were synthesised in yields ranging from 50% to 70% and their cytotoxicity against colon cancer cells (Caco-2) and the parasite Leishmania infantum determined using the MTT assay. Cytotoxicity within Caco-2 cells was manifested with IC 50 values between 0.3 and 22 μM. Compounds with the central longer alkyl chains exhibited the highest cytotoxicity. Against L. infantum, IC 50 values were encompassed within a narrower concentration range of 0.47–1.54 μM. In the parasites, the presence of nitrogen in the central chain and the length of the central alkyl chains did not especially enhance cytotoxicity. This may be due to the way these compounds are transported in the cells.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2006.09.031