دورية أكاديمية
Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate.
| العنوان: | Combined inhibition of the EGFR/AKT pathways by a novel conjugate of quinazoline with isothiocyanate. |
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| المؤلفون: | TAROZZI, ANDREA, MARCHETTI, CHIARA, NICOLINI, BENEDETTA, D'AMICO, MASSIMO, TICCHI, NICOLE, PRUCCOLI, LETIZIA, TUMIATTI, VINCENZO, SIMONI, ELENA, MILELLI, ANDREA, MINARINI, ANNA, Lodola, A, Mor, M |
| المساهمون: | Tarozzi, A, Marchetti, C, Nicolini, B, D'Amico, M, Ticchi, N, Pruccoli, L, Tumiatti, V, Simoni, E, Lodola, A, Mor, M, Milelli, A, Minarini, A. |
| سنة النشر: | 2016 |
| المجموعة: | IRIS Università degli Studi di Bologna (CRIS - Current Research Information System) |
| مصطلحات موضوعية: | EGFR-TK inhibitors Multitarget agents Sulforaphane Isothiocyanate Akt phosphorylation |
| الوصف: | 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. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | STAMPA |
| اللغة: | English |
| العلاقة: | info:eu-repo/semantics/altIdentifier/pmid/27135370; info:eu-repo/semantics/altIdentifier/wos/WOS:000376837800023; volume:117; firstpage:283; lastpage:291; numberofpages:9; journal:EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; http://hdl.handle.net/11585/580075Test; info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-84964743027 |
| DOI: | 10.1016/j.ejmech.2016.04.002 |
| الإتاحة: | https://doi.org/10.1016/j.ejmech.2016.04.002Test http://hdl.handle.net/11585/580075Test |
| رقم الانضمام: | edsbas.E2911496 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1016/j.ejmech.2016.04.002 |
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