22329-75-5Relevant articles and documents
Unsaturated carbonyl compounds and their preparation method and application
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Paragraph 0223-0230, (2019/07/04)
The invention discloses a unsaturated carbonyl compounds and their preparation method and application. The unsaturated carbonyl compounds of the general formula as the molecular structure of the following formula (I) as shown: The unsaturated carbonyl com
Synthesis of polymeric ladders by topochemical polymerization
Hou, Xiaodong,Wang, Zhihan,Lee, Joseph,Wysocki, Erin,Oian, Casey,Schlak, Jennifer,Chu, Qianli R.
supporting information, p. 1218 - 1220 (2014/02/14)
Two polymeric ladders were synthesized by topochemical polymerization. The critical assemblies with multiple reactive centers were characterized by single crystal X-ray diffraction. Approximately 64% and 70% of the mass of the two polymeric ladders can be
Mining the Cinnabaramide Biosynthetic Pathway to Generate Novel Proteasome Inhibitors
Rachid, Shwan,Huo, Liujie,Herrmann, Jennifer,Stadler, Marc,Koepcke, Baerbel,Bitzer, Jens,Mueller, Rolf
, p. 922 - 931 (2012/02/15)
The cinnabaramides and salinosporamides are mixed PKS/NRPS natural products isolated from a terrestrial streptomycete and a marine actinomycete, respectively. They interfere with the proteasome and thus potentially inhibit the growth of cancer cells. The compounds exhibit a γ-lactam-β-lactone bicyclic ring structure attached to a cyclohexenyl unit and a PKS side chain. As a first step towards improving anticancer activity and permitting genetic approaches to novel analogues, we have cloned and characterized the cinnabaramide biosynthetic genes from Streptomyces sp. JS360. In addition to the expected PKS and NRPS genes, the cluster encodes functionalities for the assembly of the hexyl side chain precursor. The corresponding enzymes exhibit relaxed substrate specificities towards a number of synthesized precursors, enabling production of novel chlorinated cinnabaramides. These were isolated and analyzed for activity, revealing that derivatives bearing a chlorine atom in the PKS side chain show higher inhibitory potentials towards the proteasome's proteolytic subunits (especially the trypsin and chymotrypsin units) and higher cytotoxicities towards human tumor cell lines than the parent cinnabaramide A. Although their activities towards the proteasome were weaker than that of salinosporamide A, the cinnabaramides were found to inhibit the growth of various fungi with greater potency. Copyright