Literature DB >> 17010616

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

João Oliveira1, Lynda Ralton, Joana Tavares, Anabela Codeiro-da-Silva, Charles S Bestwick, Anne McPherson, Paul Kong Thoo Lin.   

Abstract

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 microM. 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 microM. 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.

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Year:  2006        PMID: 17010616     DOI: 10.1016/j.bmc.2006.09.031

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  5 in total

1.  In vitro and in vivo anticancer activity of a novel nano-sized formulation based on self-assembling polymers against pancreatic cancer.

Authors:  Clare Hoskins; Mehdi Ouaissi; Sofia Costa Lima; Woei Ping Cheng; Inês Loureirio; Eric Mas; Dominique Lombardo; Anabela Cordeiro-da-Silva; Ali Ouaissi; Paul Kong Thoo Lin
Journal:  Pharm Res       Date:  2010-09-25       Impact factor: 4.200

Review 2.  Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.

Authors:  Advait S Nagle; Shilpi Khare; Arun Babu Kumar; Frantisek Supek; Andriy Buchynskyy; Casey J N Mathison; Naveen Kumar Chennamaneni; Nagendar Pendem; Frederick S Buckner; Michael H Gelb; Valentina Molteni
Journal:  Chem Rev       Date:  2014-11-03       Impact factor: 60.622

3.  Activity of Bisnaphthalimidopropyl Derivatives against Trypanosoma brucei.

Authors:  Nuno A G Graça; Luis Gaspar; David M Costa; Inês Loureiro; Paul Kong Thoo-Lin; Isbaal Ramos; Meritxell Roura; Alain Pruvost; Ian K Pemberton; Hadjer Loukil; Jane MacDougall; Joana Tavares; Anabela Cordeiro-da-Silva
Journal:  Antimicrob Agents Chemother       Date:  2016-03-25       Impact factor: 5.191

Review 4.  Novel lead compounds in pre-clinical development against African sleeping sickness.

Authors:  Michael Berninger; Ines Schmidt; Alicia Ponte-Sucre; Ulrike Holzgrabe
Journal:  Medchemcomm       Date:  2017-07-31       Impact factor: 3.597

5.  Novel Synthetic Approaches for Bisnaphthalimidopropyl (BNIP) Derivatives as Potential Anti-Parasitic Agents for the Treatment of Leishmaniasis.

Authors:  Elif Keskin; Mehmet Hikmet Ucisik; Bilgesu Onur Sucu; Mustafa Guzel
Journal:  Molecules       Date:  2019-12-16       Impact factor: 4.411

  5 in total

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