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

• Type: Article in International Scientific Journal
• Date: 2007

Authors

Jodo Oliveira (Author) Other; Lynda Ralton (Author) Other; Joana Tavares (Author) FFUP; Anabela Codeiro da Silva (Author) FFUP; Charles S Bestwick (Author) Other; Anne McPherson (Author) Other; Paul Kong Thoo Lina (Author) Other

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 15

Pages: 541-545

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 20 Citations

ISI Web of Science

Scopus - 25 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

CORDIS: Health sciences

Other information

Authenticus ID: P-004-CMH

DOI: 10.1016/j.bmc.2006.09.031

Resumo (PT): 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 IC50 values between 0.3 and 22 lM. Compounds with the central longer alkyl chains exhibited the highest cytotoxicity. Against L. infantum, IC50 values were encompassed within a narrower concentration range of 0.47–1.54 lM. 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 compoun transported in the cells. <br> <br> <a target="_blank" href="http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6TF8-4M0J4DK-C&_user=2460038&_coverDate=01%2F01%2F2007&_rdoc=56&_fmt=high&_orig=browse&_srch=doc-info(%23toc%235220%232007%23999849998%23637317%23FLA%23display%23Volume)&_cdi=5220&_sort=d&_docanchor=&_ct=62&_acct=C000057398&_version=1&_urlVersion=0&_userid=2460038&md5=3d43af542c1b7a59b0dd3a4b912f4032"> Texto integral </a> <br>

Abstract (EN): 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 IC50 values between 0.3 and 22 mu M. Compounds with the central longer alkyl chains exhibited the highest cytotoxicity. Against L. infantum, IC50 values were encompassed within a narrower concentration range of 0.47-1.54 mu M. 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 5