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Archive for the ‘Trophy Targets’ Category

Anti-protozoal cristaxenicin A

Posted by naturalproductman on November 19, 2012

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).

crystaxenicin A

JOC paper

Posted in Anti-protozoal, Diseases, Trophy Targets | Leave a Comment »

Macropalau’amine to palau’amine

Posted by naturalproductman on August 26, 2011

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.

TFA

JACS paper

Posted in Alkaloids, Methodology, Ring forming, Trophy Targets | Leave a Comment »

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

Posted by naturalproductman on August 10, 2011

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).

prostate

JNP paper

Posted in Cancer, prostate, Triterpenoids, Trophy Targets | Leave a Comment »

Stelleralides

Posted by naturalproductman on May 12, 2011

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.

sterlleralide

OL paper

Posted in Daphnane, Diseases, Diterpene, HIV, Trophy Targets | Leave a Comment »

JBIR-22

Posted by naturalproductman on February 24, 2010

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.

jbir-22

JNP paper

Posted in Trophy Targets | Leave a Comment »

Total Synthesis of Palau’amine

Posted by naturalproductman on December 30, 2009

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

Posted in Alkaloids, Cascade Reactions, Methodology, Trophy Targets | Leave a Comment »

Palau’amine

Posted by naturalproductman on February 27, 2009

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

Posted in Alkaloids, Trophy Targets | Leave a Comment »

Vinigrol

Posted by naturalproductman on February 7, 2009

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

Posted in Diterpenoids, Trophy Targets | Leave a Comment »

Englerin has selective inhibition against kidney cancer

Posted by naturalproductman on February 4, 2009

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.
englerin
check it out

Posted in Sesquiterpenes, Seven-Membered Rings, Trophy Targets | Leave a Comment »

 
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