학술논문
A Trifluorinated Thiazoline Scaffold Leading to Pro-apoptotic Agents Targeting Prohibitins.
Document Type
Article
Author
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
Source
Subject
*MOLECULES
*THIAZOLINES
*APOPTOSIS
*PURIFICATION of flue gases
*PROHIBITIN
*PHYSIOLOGY
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Language
ISSN
1433-7851
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. [ABSTRACT FROM AUTHOR]