Synthesis and antiproliferative activity of a natural like glycoconjugate polycyclic compound
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- 作者：Benedetta Maggioa ; Maria Valeria Raimondia ; Demetrio Raffaa ; Fabiana Plesciaa ; Marie-Christine Scherrmannd ; Nicolò ; Prosad ; Marianna Lauricellac ; Antonella D&rsquo ; Anneob ; Giuseppe Daidonea ; giuseppe.daidone@unipa.it" class="auth_mail" title="E-mail the corresponding author
- 关键词：O-glycoconjugate polycyclic compound ; Pyrazolo[3 ; 4-b]pyrazolo[3&prime ; 4&prime ; 2 ; 3]azepino[4 ; 5-f]azocine ; Antiproliferative activity ; MDA-MB231 ; G2/M phase arrest ; p21WAF1 inhibitor
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：21 October 2016
- 年：2016
- 卷：122
- 期：Complete
- 页码：247-256
- 全文大小：1886 K
文摘
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A natural like O-glycoconjugate polycyclic compound 4 was synthesized.
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Derivative 4 was evaluated by NCI for its in vitro antiproliferative activity.
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It caused 50% growth inhibition in the range 0.47–5.43 μM.
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Compound 4 treatment induced a prolonged arrest of MDA-MB-231 cells at G2/M phase.
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This is due to cyclin B1 and cdc2 down-regulation and p21 expression up-regulation.