Journal
ORGANIC LETTERS
Volume 15, Issue 2, Pages 322-325Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol3032363
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Funding
- Ministry of Education, Culture, Sports, Science, and Technology of Japan [22310138, 22406001]
- Astellas Foundation for Research on Metabolic Disorders
- Uehara Memorial Foundation
- Grants-in-Aid for Scientific Research [22310138, 25108719, 22406001, 25293025] Funding Source: KAKEN
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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 IC50 values of 2.0-55 mu M. Among them, siladenoserinol A and B exhibited the strongest inhibition with an IC50 value of 2.0 mu M.
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