Siladenoserinols A鈥揕: New Sulfonated Serinol Derivatives from a Tunicate as Inhibitors of p53鈥揌dm2 Interaction

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• 作者：Yuichi Nakamura ; Hikaru Kato ; Tadateru Nishikawa ; Noriyuki Iwasaki ; Yoshiaki Suwa ; Henki Rotinsulu ; Fije Losung ; Wilmar Maarisit ; Remy E. P. Mangindaan ; Hiroshi Morioka ; Hideyoshi Yokosawa ; Sachiko Tsukamoto
• 刊名：Organic Letters
• 出版年：2013
• 出版时间：January 18, 2013
• 年：2013
• 卷：15
• 期：2
• 页码：322-325
• 全文大小：286K
• 年卷期：v.15,no.2(January 18, 2013)
• ISSN：1523-7052

文摘

Siladenoserinols A鈥揕 were isolated from a tunicate as inhibitors of p53鈥揌dm2 interaction, a promising target for cancer chemotherapy. Their structures including the absolute configurations were elucidated to be new sulfonated serinol derivatives, each of which contains a 6,8-dioxabicyclo[3.2.1]octane unit and either glycerophosphocholine or glycerophosphoethanolamine moiety. They inhibited p53鈥揌dm2 interaction with IC₅₀ values of 2.0鈥?5 渭M. Among them, siladenoserinol A and B exhibited the strongest inhibition with an IC₅₀ value of 2.0 渭M.