We report herein the synthesis and biol. evaluation of novel deoxynucleoside-​bile acid conjugates linked through a 1,​2,​3-​triazole ring. The conjugates were synthesized via Cu(i) mediated 1,​3-​dipolar cycloaddn. reaction ('click' chem.) of 3-​azido bile acid derivs. and terminal alkyne moieties linked to the C-​8 position of deoxyadenosine. All novel mols. were evaluated in vitro for their anti-​proliferative activity against four human cell lines (i.e., leukemic T Jurkat and K562; colon carcinoma HCT116; and ovarian cancer A2780) and their cytotoxicity toward human fibroblast cells. Several conjugates exhibited strong anti-​proliferative activity against human leukemia T cells. The best cytotoxicity was obsd. for HdA-​CDC on both leukemia cell lines with IC50 up to 8.51 μM. The apoptotic activity of several conjugates was also established.

Synthesis and in vitro cytotoxicity of deoxyadenosine-​bile acid conjugates linked with 1,​2,​3-​triazole

PERRONE, Daniela;BORTOLINI, Olga;FOGAGNOLO, Marco;MARCHESI, Elena;MARI, Lara;MASSARENTI, Chiara;SFORZA, Fabio;VARANI, Katia;
2013

Abstract

We report herein the synthesis and biol. evaluation of novel deoxynucleoside-​bile acid conjugates linked through a 1,​2,​3-​triazole ring. The conjugates were synthesized via Cu(i) mediated 1,​3-​dipolar cycloaddn. reaction ('click' chem.) of 3-​azido bile acid derivs. and terminal alkyne moieties linked to the C-​8 position of deoxyadenosine. All novel mols. were evaluated in vitro for their anti-​proliferative activity against four human cell lines (i.e., leukemic T Jurkat and K562; colon carcinoma HCT116; and ovarian cancer A2780) and their cytotoxicity toward human fibroblast cells. Several conjugates exhibited strong anti-​proliferative activity against human leukemia T cells. The best cytotoxicity was obsd. for HdA-​CDC on both leukemia cell lines with IC50 up to 8.51 μM. The apoptotic activity of several conjugates was also established.
2013
Perrone, Daniela; Bortolini, Olga; Fogagnolo, Marco; Marchesi, Elena; Mari, Lara; Massarenti, Chiara; Navacchia M., L; Sforza, Fabio; Varani, Katia; Capobianco, M. L.
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/1882518
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 13
  • ???jsp.display-item.citation.isi??? 13
social impact