2. Academic Validation
  3. In vitro optimization of non-small cell lung cancer activity with troxacitabine, L-1,3-dioxolane-cytidine, prodrugs

In vitro optimization of non-small cell lung cancer activity with troxacitabine, L-1,3-dioxolane-cytidine, prodrugs

  • J Med Chem. 2007 May 3;50(9):2249-53. doi: 10.1021/jm0612923.
Marco Radi 1,  Auke D Adema,  Jonathan R Daft,  Jong H Cho,  Eveline K Hoebe,  Lou-Ella M M Alexander,  Godefridus J Peters,  Chung K Chu
Affiliations

Affiliation

  • 1 The University of Georgia College of Pharmacy, Athens, Georgia 30602, USA.
PMID: 17419604 DOI: 10.1021/jm0612923
Abstract

l-1,3-Dioxolane-cytidine, a potent Anticancer agent against leukemia, has limited efficacy against solid tumors, perhaps due to its hydrophilicity. Herein, a library of prodrugs were synthesized to optimize in vitro antitumor activity against non-small cell lung Cancer. N4-Substituted fatty acid amide prodrugs of 10-16 carbon chain length demonstrated significantly improved antitumor activity over l-1,3-dioxolane-cytidine. These in vitro results suggest that the in vivo therapeutic efficacy of l-1,3-dioxolane-cytidine against solid tumors may be improved with prodrug strategies.

Figures