Synthesis and in vitro antiproliferative activities of (5-aryl-1,2,4-oxadiazole-3-yl)methyl D-ribofuranosides

ROMINA E. AVANZO; JOSÉ M. PADRÓN; NORMA B. D´ACCORSO; MIRTA L. FASCIO

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

PERGAMON-ELSEVIER SCIENCE LTD

Año: 2017 vol. 27 p. 3674 - 3677

0960-894X

The emergence of multidrug resistance cell lines is one of the major obstacles in the success of cancer chemotherapeutic treatment. Therefore, it remains a big challenge the development of new and effective drugs to defeat cancer. The presence of nitrogen heterocycles in the architectural design of drugs has led to the discovery of new leading compounds. Herein, we report the synthesis, characterization and in vitro antiproliferative activity against six cancer cell lines of D-ribofuranosides derivatives bearing a 1,2,4-oxadiazolic ring, with the aim of developing new active compounds. Most of these derivatives exhibit significant antiproliferative activities in the micromolar range. Noteworthy, the most potent compound of the series showed better selectivity towards the more resistant colon cancer cell line WiDr.