Title:
BISNAPHTHALIMIDOPROPYL DERIVATIVE COMPOUNDS WITH ANTI-PARASITE AND ANTI-CANCER ACTIVITY
Document Type and Number:
WIPO Patent Application WO2008007262
Kind Code:
B1
Abstract:
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 IC50 values between 0.3 and 22 m M after 48h of compounds incubation. Against Leishmania infantum, IC50 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.
Inventors:
CORDEIRO DA SILVA ANABELA (PT)
PINTO DA COSTA TAVARES JOANA ALEXANDRA (PT)
KONG THOO LIN PAUL (GB)
PINTO DA COSTA TAVARES JOANA ALEXANDRA (PT)
KONG THOO LIN PAUL (GB)
Application Number:
PCT/IB2007/052311
Publication Date:
October 09, 2008
Filing Date:
June 15, 2007
Export Citation:
Assignee:
UNIV DO PORTO (PT)
CORDEIRO DA SILVA ANABELA (PT)
PINTO DA COSTA TAVARES JOANA ALEXANDRA (PT)
KONG THOO LIN PAUL (GB)
CORDEIRO DA SILVA ANABELA (PT)
PINTO DA COSTA TAVARES JOANA ALEXANDRA (PT)
KONG THOO LIN PAUL (GB)
International Classes:
C07D221/14; A61K31/473; A61P33/02; A61P33/06; A61P35/00
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