摘要 |
The bisnaphthalimidopropyl derivatives with anti-parasitic and anti-cancer activity. Bisnaphthalimidopropyl derivatives (A) BNIPPut, BNIPDapen, BNIPDhex, BNIPDahep, BNIPDaoct, BNIPDanon, BNTPDadec, BNIPDadod, BNPDpta, BNIPDeta were synthesized in yields ranging from 50-70 and their cytotoxicity against colon cancer cells (CaCo-2) and the parasite Leishmania infantum determined using the MTT assay and by luciferase activity present in parasite, respectively. Cytotoxicity within CaCo-2 cells was manifested with IC<SUB>50</SUB> values between 0.3 and 22 m M after 48h of compounds incubation. Against Leishmania infantum, IC<SUB>50</SUB> values were encompassed within a narrower concentration range of 0.39-2.09 m M, for pro- mastigote form, and between 5.24 and 17.42 m M, for axenic amastigote and between 2.43 and 9.52 m M, for intracellular amastigote forms. These compounds can be an alternative to the normal therapeutic in the fields below (A), could be a solution to the toxicity and resistance related to the compounds existent in the market. Point of diversity. |
申请人 |
UNIVERSIDADE DO PORTO;CORDEIRO DA SILVA, ANABELA;PINTO DA COSTA TAVARES, JOANA ALEXANDRA;KONG THOO LIN, PAUL |
发明人 |
CORDEIRO DA SILVA, ANABELA;PINTO DA COSTA TAVARES, JOANA ALEXANDRA;KONG THOO LIN, PAUL |