Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 81, Issue -, Pages 181-191Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.05.014
Keywords
Benzofuran; Cytotoxicity; mTOR; Cancer; Rapamycin
Categories
Funding
- region Alsace
- MNESR
- SATT Ile-de-France Innov
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A series of 32 derivatives and isosteres of the mTOR inhibitor 2 were synthesized and compared for their cytotoxicity in radioresistant SQ20B cancer cell line. Several of these compounds, in particular 30b, were significantly more cytotoxic than 2. Importantly, 30b was shown to block both mTORC1 and Akt signaling, suggesting insensitivity to the resistance associated to Akt overactivation observed with rapamycin derivatives currently used in clinic. (C) 2014 Elsevier Masson SAS. All rights reserved.
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