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 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.
Oliveira
João
J
The Robert Gordon University, School of Life Sciences, St. Andrew Street, Aberdeen AB25 1HG, Scotland, UK.
Ralton
Lynda
L
Tavares
Joana
J
Codeiro-da-Silva
Anabela
A
Bestwick
Charles S
CS
McPherson
Anne
A
Thoo Lin
Paul Kong
PK
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000977:Antiparasitic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018938:Caco-2 Cells; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D018314:Leishmania infantum / Q000187:drug effects; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D011073:Polyamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D000977:Antiparasitic Agents; D011073:Polyamines