Differential effect of heterocyclic d-ribofuranoside derivatives on human prostate cancer cell viability and cell cycle progression

Gueron, Geraldine; Avanzo, Romina Edith; Schuster, Federico; Carabelos, María Noelia; Vázquez, Elba S.; Fascio, Mirta L.; D’Accorso, Norma B.

doi:10.1016/j.biopha.2014.08.010

Cited by 5 publications

(1 citation statement)

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“…4 Our previous efforts to obtain effective antitumor agents showed that 5-deoxy-5-S-(1,2,4-triazol-3-yl)-2,3-O-cyclopentylidene-β-D-ribofuranoside derivatives 1-4 ( Figure 1) had a moderate inhibitory activity against BW 5147 lymphoma cell line (1-2) 5 and prostate cancer cell line (PC3) (1-4). 6 In the latter, compounds 1, 3 and 4 were found to arrest cells at the G 0 /G 1 phase of the cell cycle, while compound 2 induced apoptosis. In these cases, five-membered heterocyclic rings of known medicinal relevance (triazole, isoxazole and isoxazoline) 7 were selected to synthesize the novel diheterocyclic Dribofuranoside derivatives 1-4.…”

Section: Bioorganic and Medicinal Chemistry Lettersmentioning

confidence: 97%

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

Avanzo

Padrón

D’Accorso

et al. 2017

Bioorganic & Medicinal Chemistry Letters

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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.

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