Abstract

Lubeluzole, a neuroprotective anti-ischemic drug, and its enantiomer were prepared following a convenient procedure based on hydrolytic kinetic resolution. The ee values were >99% and 96%, respectively, as assessed by HPLC analysis. The chemosensitizing effects of both enantiomers were evaluated in combination with either doxorubicin (human ovarian adenocarcinoma A2780 cells) or paclitaxel (human lung carcinoma A549 cells) by the MTT assay. At the lowest concentrations used, lubeluzole showed an overall and remarkable tendency to synergize with both anticancer drugs. In ovarian cancer cells a clear prevalence of antagonistic effect was observed for the R-enantiomer. The synergistic effects of lubeluzole for both drugs were observed over a wide concentration window (0.005–5 lM), the lowest limit being at least 40 times lower than human plasma concentrations previously reported as causing serious side effects.

Autore Pugliese

• Carocci Alessia , Catalano Alessia , Carrieri Antonio , Franchini Carlo , Lentini Giovanni , Cavalluzzi Maria Maddalena

Tutti gli autori

• CAROCCI A.;CATALANO A.;CARRIERI A.;FRANCHINI C.;LENTINI G.;CAVALLUZZI M.M.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2013

ISSN

0960-894X

ISBN

Non Disponibile

Numero di citazioni Wos

9

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

10

Ultimo Aggiornamento Citazioni

Non Disponibile

Settori ERC

Non Disponibile

Codici ASJC

Non Disponibile