Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Privileged 1,2,4-Oxadiazoles in Anticancer Drug Design: Novel 5- Aryloxymethyl-1,2,4-oxadiazole Leads for Prostate Cancer Therapy

Author(s): Alexey Lukin, Ruben Karapetian, Yan Ivanenkov, Mikhail Krasavin.

Graphical Abstract:


Based on the structure of the previously identified leads, new series of compounds containing 1,2,4-oxadiazole core was designed. A small, diverse library of 51 compounds including both 2-(acylamino)ethyl and 2-ureidoethyl side chains was synthesized using parallel chemistry and tested for antiproliferative activity against prostate cancer DU-145 cell line. Four hit compounds – all belonging to 2-ureidoethyl series – were identified and three compounds were confirmed as 10-20 µM inhibitors. The similarity in compounds’ periphery and the data obtained previously suggest a similar mode of action for these compounds which was postulated as tubulin inhibition and was confirmed by in silico docking. These data provide further evidence for the privileged character of 1,2,4-oxadiazoles in antiproliferative compound design.

Keywords: 1, 2, 4-oxadiazoles, privileged structures, prostate cancer, DU-145 cell line, hit rate, tubulin inhibitors, colchicines binding site, in silico docking.

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Article Details

Year: 2016
Page: [198 - 204]
Pages: 7
DOI: 10.2174/1570180812999150812164251
Price: $58