HIV-1 reverse transcriptase structure with catechol diether

Karen Anderson and co-workers at Yale have reported in JACS on a crystal structures of HIV-1 reverse transcriptase with catechol diether drugs.

JACS paper

Aetheramides A and B

Rolf Mueller and co-workers at Universität des Saarlandes have reported in Organic Letters on some anti-HIV depsipeptides with 15 nM IC50 values.

OL paper

Oxyingenol synthesis

Hideo Kigoshi and co-workers from the University of Tsukuba have reported in ACIE on the synthesis of oxyingenol.

ACIE paper

Anti-HIV schilancitrilactone

Han-Dong Sun and co-workers from the Kunming Institute of Botany have reported in Organic Letters on the isolation of schilancitrilactones A-C.

OL paper

Daphnane diterpenes

Matthias Hamburger and co-workers from the University of Basel in Switzerland have reported in JNP on the anti-HIV activities of some daphnane derived natural products.

JNP paper

Video games and protein structures

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

EFdA synthesis

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).

OL paper

Salviadione synthesis

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.

Tetrahedron 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

Inactive Analog

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.

European JOC paper