Naturalproductman’s Blog

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Archive for the ‘HIV’ Category

Video games and protein structures

Posted by naturalproductman on September 20, 2011

David Baker and co-workers at the University of Washington have reported in Nature Structral and Molecular Biology on the structure of an HIV protease enzyme.  Their approach involved the use of a video game called Foldit.

Nature Structural and Molecular Biology

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Posted in Computational, Diseases, Enzymes, HIV, M-PMV (Mason-Pfizer monkey virus) retroviral protease, Molecular modeling, Protein Targets, Proteins | Leave a Comment »

EFdA synthesis

Posted by naturalproductman on September 4, 2011

Shigefumi Kuwahara and co-workers from Tohoku University have reported in Organic Letters on their synthesis of an anti-HIV compound, 4′-ethynyl-2-fluoro-2′-deoxyadenosine (EFdA).

HIV

OL paper

Posted in Diseases, HIV, Methodology, Nucleic acids, Total Synthesis | Leave a Comment »

Salviadione synthesis

Posted by naturalproductman on June 9, 2011

Bjorn Soderberg and co-workers at West Virginia University have reported in Tetrahedron on a synthesis of salviadione with the key reaction being a palladium mediated C-N bond formation.

salviadione

Tetrahedron paper

Posted in Alkaloids, Aromatic, Cascade Reactions, Diseases, HIV, Methodology, Palladium, Transition Metal | 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 »

Inactive Analog

Posted by naturalproductman on January 24, 2011

Piet Herdewijn and co-worker at the Katholieke Universiteit Leuven in Belgium have reported on a nucleoside analog in the hopes of uncovering anti-HCV activity.  Unfortunately however, this compound did not have any biological activity.  You might think that this information is not good because it didn’t have biological activity – but to a computational chemist, who is familiar with QSAR (quantitative structure activity relationships) and COMFA, COMSIA and other computer aided drug design techniques, this information is indeed valuable.  The paper does mention however a biologically active  nucleoside analog (a natural product), C-branched nucleoside oxetanocin A, that has a four membered ring instead of the usual ribose ring.

anti HCV

European JOC paper

Posted in Diseases, HIV, Methodology, Nucleic acids, Unnatural Products | Leave a Comment »

Didemnaketal Synthesis

Posted by naturalproductman on October 29, 2010

Haruhiko Fuwa and co-workers from Tohoku University have published in Organic Letters on a synthesis of didemnaketal which has an IC50 value of 1 micromolar against HIV-1 protease.  The spiroketal unit was accessed from a PPTS catalyzed condensation of an alcohol and a dihydropyran.

spiroketal

 

OL paper

Posted in Cascade Reactions, cross coupling, Diseases, HIV, Methodology, Palladium, Polyketides, Spiroketals, Suzuki-Miyaura, Transition Metal | Leave a Comment »

Baculiferins A-O

Posted by naturalproductman on July 27, 2010

Wenhan Lin and co-workers from Peking University have published on the isolation of some pyrrole alkaloids.  Baculiferin M had an IC50 of 0.2 micrograms/mL against HIV-1 IIIB virus expressed in MAGI cells.

baculiferins

Bioorganic and Medicinal Chemistry paper

Posted in Alkaloids, Diseases, HIV | Leave a Comment »

Reactivate HIV with Diterpenes

Posted by naturalproductman on February 10, 2010

Fernando Echeverri and co-workers at Universidad de Antioquia have recently published in Phytochemistry on some diterpenes that reactivate HIV.

hiv

Phytochemistry paper

Posted in Diseases, Diterpene, HIV | Leave a Comment »