Callyspongiamides A and B, sterol O-acyltransferase inhibitors, from the Indonesian marine sponge Callyspongia sp

[Display omitted] Callyspongiamides A (1) and B (2), two new sterol O-acyltransferase (SOAT) inhibitors, were isolated from the Indonesian marine sponge Callyspongia sp. together with a known congener, dysamide A (3). The structures of 1 and 2 were elucidated to be polychlorine-containing modified d...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2018-06, Vol.28 (10), p.1911-1914
Main Authors: Kapojos, Magie M., Abdjul, Delfly B., Yamazaki, Hiroyuki, Ohshiro, Taichi, Rotinsulu, Henki, Wewengkang, Defny S., Sumilat, Deiske A., Tomoda, Hiroshi, Namikoshi, Michio, Uchida, Ryuji
Format: Article
Language:English
Subjects:
Animals
Callyspongia - chemistry
Callyspongia - metabolism
Callyspongiamide
Dipeptides - chemistry
Dipeptides - isolation & purification
Dipeptides - pharmacology
Enzyme Assays
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - isolation & purification
Enzyme Inhibitors - pharmacology
Indonesia
Inhibitor
Inhibitory Concentration 50
Isoenzymes - antagonists & inhibitors
Isoenzymes - metabolism
Magnetic Resonance Spectroscopy
Marine sponge Callyspongia sp
Molecular Conformation
Polychlorine-containing modified dipeptide
Sterol O-acyltransferase
Sterol O-Acyltransferase - antagonists & inhibitors
Sterol O-Acyltransferase - metabolism
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Summary:[Display omitted] Callyspongiamides A (1) and B (2), two new sterol O-acyltransferase (SOAT) inhibitors, were isolated from the Indonesian marine sponge Callyspongia sp. together with a known congener, dysamide A (3). The structures of 1 and 2 were elucidated to be polychlorine-containing modified dipeptides based on their spectroscopic data. Compounds 1–3 inhibited both of the SOAT isozymes, SOAT1 and SOAT2, in cell-based and enzyme-based assays.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2018.03.077