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Wiley, Angewandte Chemie, 38(126), p. 10314-10318, 2014

DOI: 10.1002/ange.201405758

Wiley, Angewandte Chemie International Edition, 38(53), p. 10150-10154, 2014

DOI: 10.1002/anie.201405758

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A Trifluorinated Thiazoline Scaffold Leading to Pro-apoptotic Agents Targeting Prohibitins

This paper is available in a repository.
This paper is available in a repository.

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Abstract

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.