Literature DB >> 28716494

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

Romina E Avanzo1, José M Padrón2, Norma B D'Accorso3, Mirta L Fascio4.   

Abstract

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-ribofuranoside 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.
Copyright © 2017 Elsevier Ltd. All rights reserved.

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Keywords:  1,2,4-Oxadiazole; 1,2,4-Triazole; 5-Amino-1,3,4-thiadiazole; Antiproliferative activity; d-Ribose

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Year:  2017        PMID: 28716494     DOI: 10.1016/j.bmcl.2017.07.015

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

Review 1.  Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds.

Authors:  Alessandra Benassi; Filippo Doria; Valentina Pirota
Journal:  Int J Mol Sci       Date:  2020-11-18       Impact factor: 5.923

  1 in total

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