Anti-protozoal cristaxenicin A

Yoichi Nakao and co-workers from Waseda University have reported in JOC on the isolation of cristaxenicin A, which had activities against Leishmania amazonensis (IC₅₀ value of 0.088 μM) and Trypanosoma congolense (IC₅₀ value of 0.25 μM).

JOC paper

Macropalau’amine to palau’amine

Phil Baran and co-workers have reported in JACS on their syntheses of axinellamines, palau’amine and massadines.  The key step to access palau’amine was the macropalau’amine intermediate, which closes under acidic conditions to form the final hexacyclic ring system.

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

Stelleralides

Kuo-Hsiung Lee and co-workers at the University of North Carolina have reported in Organic Letters on the isolation of a very potent anti-HIV compound stelleralide A, which had an EC90 of 0.4 nM.

OL paper

JBIR-22

Kazuo Shin-ya and co-workers at National Institute of Advanced Industrial Science and Technology in Japan have recently published in the Journal of Natural Products of the isolation of JBIR-22.  This pyrrolidinedione was found to be an analogue of equisetin, which has protein protein interaction inhibitory qualities.  They isolated the species that produced this compound (Verticillium sp. f21794) by treating the soil sample with anthracycline antibiotic, daunomycin, which helped them isolate the slower growing fungi from a mix of fast- and slow-growing fungi.

JNP paper

Total Synthesis of Palau’amine

Someone was bound to do it, but wow – Phil Baran and co-workers have synthesized palau’amine recently and reported their route in ACIEE.

ACIEE paper

Palau’amine

Palau’amine, isolated by the group of the late Paul Scheuer in the University of Hawaii at Manoa in 1993, is still a desirable target for synthetic chemists around the world.  Many people are working on it and it has yet to be synthesized by anybody.  The stereochemistry of the cyclopentane core is controversial.  It is an oroidin dimer natural product just like massadine, however, massadine has been synthesized by the Baran group at Scripps last year.

JACS isolation

Vinigrol

This natural product has been around for over 20 years and a research group has yet to synthesize it. It’s a very challenging structure and so cool. Some day someone will make it.

isolation of vinigrol

Englerin has selective inhibition against kidney cancer

This molecule has one of the most interesting activities I’ve ever seen.  Its selective activity toward renal cancer cell lines is quite intriguing.  Something else to note is its tricyclic core including a seven membered ring.  The molecule was isolated from phyllanthus engleri, a plant found in Africa.

check it out