Benzofuran derivatives as anticancer inhibitors of mTOR signaling.

Details

Serval ID
serval:BIB_17A8F8E37C36
Type
Article: article from journal or magazin.
Collection
Publications
Title
Benzofuran derivatives as anticancer inhibitors of mTOR signaling.
Journal
European Journal of Medicinal Chemistry
Author(s)
Salomé C., Ribeiro N., Chavagnan T., Thuaud F., Serova M., de Gramont A., Faivre S., Raymond E., Désaubry L.
ISSN
1768-3254 (Electronic)
ISSN-L
0223-5234
Publication state
Published
Issued date
2014
Peer-reviewed
Oui
Volume
81
Pages
181-191
Language
english
Notes
Publication types: Journal Article ; Research Support, Non-U.S. Gov't Publication Status: ppublish
Abstract
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.
Pubmed
Create date
11/02/2015 12:07
Last modification date
20/08/2019 12:47
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