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A trifluorinated thiazoline scaffold leading to pro-apoptotic agents targeting prohibitins
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2014 (English)In: Angewandte Chemie International Edition, ISSN 1433-7851, E-ISSN 1521-3773, Vol. 53, no 38, p. 10150-10154Article in journal (Refereed) Published
Abstract [en]

A new class of small molecules, with an unprecedented trifluorothiazoline scaffold, were synthesized and their pro-apoptotic activity was evaluated. With an EC50 in the low micromolar range, these compounds proved to be potent inducers of apoptosis in a broad spectrum of tumor cell lines, regardless of the functional status of p53. Fast structure-activity relationship studies allowed the preparation of the strongest apoptosis-inducing candidate. Using a high performance affinity purification approach, we identified prohibitins 1 and 2, key proteins involved in the maintenance of cell viability, as the targets for these compounds.

Place, publisher, year, edition, pages
2014. Vol. 53, no 38, p. 10150-10154
Keywords [en]
antitumor agents, drug discovery, fluorine, heterocycles, medicinal chemistry
National Category
Chemical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-339266DOI: 10.1002/anie.201405758PubMedID: 25196378OAI: oai:DiVA.org:uu-339266DiVA, id: diva2:1175298
Available from: 2018-01-17 Created: 2018-01-17 Last updated: 2018-02-15Bibliographically approved

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Caja, Laia

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