A Trifluorinated Thiazoline Scaffold Leading to Pro‐apoptotic Agents Targeting Prohibitins1. (5th September 2014)

• Record Type: Journal Article
• Authors: Pérez‐Perarnau, Alba; Preciado, Sara; Palmeri, Claudia Mariela; Moncunill‐Massaguer, Cristina; Iglesias‐Serret, Daniel; González‐Gironès, Diana M.; Miguel, Miriam; Karasawa, Satoki; Sakamoto, Satoshi; Cosialls, Ana M.; Rubio‐Patiño, Camila; Saura‐Esteller, José; Ramón, Rosario; Caja, Laia; Fabregat, Isabel; Pons, Gabriel; Handa, Hiroshi; Albericio, Fernando; Gil, Joan; Lavilla, Rodolfo
• Is Part Of: Angewandte Chemie. Volume 126:Number 38(2014)
• Page Start: 10314
• Page End: 10318
• Publication Date: 2014-09-05
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/ange.201405758
• Languages: English
• ISSNs: 0044-8249

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>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.</p> </abstract>