New indolizine-chalcones as potent inhibitors of human farnesyltransferase: Design, synthesis and biological evaluation

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• 作者：Iuliana-Monica Moise^a ; Alina Ghinet^a ; ^b ; ^c ; Dalila Belei^a ; Joë ; lle Dubois^d ; Amaury Farce^c ; ^e ; Elena Bî ; cu^a ; ^{elena@uaic.ro" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Farnesyltransferase inhibitor ; Phenothiazine ; Chalcone ; Indolizine ; Antitumor agent
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 August 2016
• 年：2016
• 卷：26
• 期：15
• 页码：3730-3734
• 全文大小：798 K

文摘

A new family of indolizine–chalcones was designed, synthesized and screened for the inhibitory potential on human farnesyltransferase in vitro to identify potent antitumor agents. The most active compound was phenothiazine rong class="boldFont">2arong>, exhibiting an IC₅₀ value in the low nanomolar range, similar to that of known FTI-276, highly potent farnesyltransferase inhibitor. The newly synthesized indolizine–chalcones rong class="boldFont">2arong>–rong class="boldFont">drong> constitute the most efficient inhibitors of farnesyltransferase bearing a phenothiazine unit known to date.