- Siladenoserinols A-L: new sulfonated serinol derivatives from a tunicate as inhibitors of p53-Hdm2 interaction.
Siladenoserinols A-L: new sulfonated serinol derivatives from a tunicate as inhibitors of p53-Hdm2 interaction.
Organic letters (2012-12-28)
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
PMID23268733
摘要
Siladenoserinols A-L were isolated from a tunicate as inhibitors of p53-Hdm2 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-Hdm2 interaction with IC(50) values of 2.0-55 μM. Among them, siladenoserinol A and B exhibited the strongest inhibition with an IC(50) value of 2.0 μM.
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