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Elsevier, Bioorganic and Medicinal Chemistry Letters, 18(24), p. 4477-4481, 2014

DOI: 10.1016/j.bmcl.2014.07.089

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Antiproliferative 4-(1,2,4-oxadiazol-5-yl)piperidine-1-carboxamides, a new tubulin inhibitor chemotype

Journal article published in 2014 by Mikhail Krasavin ORCID, Andrey V. Sosnov, Ruben Karapetian, Igor Konstantinov, Olga Soldatkina, Elena Godovykh, Fedor Zubkov, Ruoli Bai, Ernest Hamel, Andrei A. Gakh
This paper is available in a repository.
This paper is available in a repository.

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Abstract

We discovered a new chemical class of antiproliferative agents, 4-(1,2,4-oxadiazol-5-yl)piperidine-1-carboxamides. SAR-guided optimization of the two distinct terminal fragments yielded a compound with 120nM potency in an antiproliferative assay. Biological activity profile studies (COMPARE analysis) demonstrated that 4-(1,2,4-oxadiazol-5-yl)piperidine-1-carboxamides act as tubulin inhibitors, and this conclusion was confirmed via biochemical assays with pure tubulin and demonstration of increased numbers of mitotic cells following treatment of a leukemia cell line.