Document Report Card

ID: ALA1141377

Journal: J Nat Prod

Title: Cinnabaramides A-G: analogues of lactacystin and salinosporamide from a terrestrial streptomycete.

Authors: Stadler M, Bitzer J, Mayer-Bartschmid A, Müller H, Benet-Buchholz J, Gantner F, Tichy HV, Reinemer P, Bacon KB.

Abstract: The cinnabaramides A-G (1-7) were isolated from a terrestrial strain of Streptomyces as potent and selective inhibitors of the human 20S proteasome. Their chemical and biological properties resemble those of salinosporamide A, a recently identified lead compound from an obligate marine actinomycete, which is currently under development as an anticancer agent. Cinnabaramides F and G (6, 7) combine essential structural features of salinosporamide A and lactacystin and show about equal potency in vitro, with IC50 values in the 1 nM range. The properties and phylogenetic position of the producer organism, the production and isolation of compounds 1-7, their structure elucidation by MS and NMR, and their biological activities are reported. Additionally, an X-ray crystal structure was obtained from cinnabaramide A (1).

CiteXplore: 17249727

DOI: 10.1021/np060162u