European Journal of Medicinal Chemistry p. 283 - 291 (2016)
Update date:2022-08-11
Topics:
Tarozzi, Andrea
Marchetti, Chiara
Nicolini, Benedetta
D'Amico, Massimo
Ticchi, Nicole
Pruccoli, Letizia
Tumiatti, Vincenzo
Simoni, Elena
Lodola, Alessio
Mor, Marco
Milelli, Andrea
Minarini, Anna
Epidermal growth factor receptor inhibitors (EGFR-TKIs) represent a class of compounds widely used in anticancer therapy. An increasing number of studies reports on combination therapies in which the block of the EGFR-TK activity is associated with inhibition of its downstream pathways, as PI3K-Akt. Sulforaphane targets the PI3K-Akt pathway whose dysregulation is implicated in many functions of cancer cells. According to these considerations, a series of multitarget molecules have been designed by combining key structural features derived from an EGFR-TKI, PD168393, and the isothiocyanate sulforaphane. Among the obtained molecules 1-6, compound 6 emerges as a promising lead compound able to exert antiproliferative and proapoptotic effects in A431 epithelial cancer cell line by covalently binding to EGFR-TK, and reducing the phosphorylation of Akt without affecting the total Akt levels.
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