Neocarzinostatin

Der-Hang Chin and co-workers at National Chung Hsing University in Taiwan have published in Chemistry a European Journal on a neat carrier protein that cyclizes neocarzinostatin, an enediyne.

 

Chemistry a European Journal paper

Maduropeptin Synthesis

From the group that brought you a synthesis of merrilactone comes another paper in JACS on the synthesis of Maduropeptin.  Osamu Hirama’s group at Tohoku University in Japan has recently published in this journal on the synthesis of a molecule, maduropeptin, that was isolated by a group from Bristol Meyers Squibb.  Maduropeptin has the ability to cleave DNA by undergoing a Bergman cyclization and forming a p-benzyne biradical, which in turn abstracts hydrogens.

JACS 2007 paper

JACS paper

Uncialamycin Progress

Nicolau has already synthesized uncialamycin.  However, just because one person has completed the synthesis, it doesn’t mean there will be more elegant ways to access the same target molecule.  This enediyne natural product was isolated from a streptomycete isolated from the surface of a lichen, Cladonia uncialis.  It has interesting anti-tumor activities.  The highlight of the synthesis from Pierre van de Weghe from the Universite de Rennes in France is the intramolecular imino-alkyne diels alder to form a subsituted quinoline.  You can check out the synthesis in JOC.

JOC paper

C-1027 Has pM Activity Against Human Hepatic Carcinoma JHH-7

From the lab of Masayuki Inoue and Masahiro Hirama in Tohoku University in Japan (the same people who synthesized merrilactone) comes this JACS article on an enediyne with very excellent IC50 at 6.1 pM for the JHH-7 cancer cell line.

JACS article