Synthesis and biological evaluation of nitric oxide-donating analogues of sulindac for prostate cancer treatment.
Bioorg Med Chem
; 22(2): 756-61, 2014 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-24387865
ABSTRACT
A series of analogues of the non-steroidal anti-inflammatory drug (NSAID) sulindac 1 were synthesised tethered to nitric oxide (NO) donating functional groups. Sulindac shows antiproliterative effects against immortal PC3 cell lines. It was previously demonstrated that the effect can be enhanced when tethered to NO releasing groups such as nitrate esters, furoxans and sydnonimines. To explore this approach further, a total of fifty-six sulindac-NO analogues were prepared and they were evaluated as NO-releasing cytotoxic agents against prostate cancer (PCa) cell lines. Compounds 1k and 1n exhibited significant cytotoxic with IC50 values of 6.1±4.1 and 12.1±3.2µM, respectively, coupled with observed nitric oxide release.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Neoplasias da Próstata
/
Sulindaco
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Antineoplásicos
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Óxido Nítrico
Limite:
Humans
/
Male
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article