Baccharin

Satoshi Endo and co-workers from Gifu Pharmaceutical University have reported in JNP on the isolation of baccharin a 17-beta-hydroxysteroid dehydrogenase inhibitor.

JNP paper

Arabilin synthesis

Kathlyn Parker and colleague have reported in JACS on a synthesis of arabilin, an androgen receptor antagonist that can potentially treat prostate cancer (IC50 of 11 micromolar towards AR).  A 1,7-hydride shift occured in their key Stille coupling to afford the correct isomer.

JACS paper

(8R)-3β,8-Dihydroxypolypoda-13E,17E,21-triene

Thomas Simmet and co-workers from Ulm University have reported in the Journal of Natural Products on the isolation of (8R)-3β,8-Dihydroxypolypoda-13E,17E,21-triene from the oleogum resin of P. lentiscus.  This compound had inhibitory activity against androgen-insensitive prostate cancers (~10 micromolar).

JNP paper

Archazolids E and F

Dirk Mensche and colleagues at Ruprecht-Karls-Universitat Heidelberg in Germany have reported in the Journal of Natural Products on the isolation of archazolids E and F.  Archazolid F had an IC50 of 0.131 nM against MCF7 breast adenocarcinoma cell lines.

JNP paper

Sterol Glycosides

Julia Kubanek and co-workers at Georgia Institute of Technology have published in Bioorganic and Medicinal Chemistry on the isolation of sterol glycosides, 19-O-β-d-glucopyranosyl-19-hydroxy-cholest-4-en-3-one (1) and 19-O-β-d-N-acetyl-2-aminoglucopyranosyl-19-hydroxy-cholest-4-en-3-one (2), which were collected from the Fijian red alga Peyssonnelia sp.  and had biological activity against human breast cancer cell lines MDA-MB-468 with IC₅₀ = 0.71 and 0.86 μM, respectively.

 

BMC paper