- Development of a non-hydroxamate dual matrix metalloproteinase (MMP)-7/-13 inhibitor
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Matrix metalloproteinase 7 (MMP-7) is a member of the MMP superfamily and is able to degrade extracellular matrix proteins such as casein, gelatin, fibronectin and proteoglycan. MMP-7 is a validated target for the development of small molecule drugs against cancer. MMP-13 is within the enzyme class the most efficient contributor to type II collagen degeneration and is a validated target in arthritis and cancer. We have developed the dual MMP-7/-13 inhibitor ZHAWOC6941 with IC50-values of 2.2 μM (MMP-7) and 1.2 μM (MMP-13) that is selective over a broad range of MMP isoforms. It spares MMP-1, -2, -3, -8, -9, -12 and -14, making it a valuable modulator for targeted polypharmacology approaches.
- Fischer, Thomas,Riedl, Rainer
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- Highly efficient preparation of selectively isotope cluster-labeled long chain fatty acids via two consecutive Csp3-Csp3 cross-coupling reactions
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An efficient synthesis involving two copper-catalyzed alkyl-alkyl coupling reactions has been designed to easily access doubly isotope-labeled fatty acids. Such NMR- and IR-active compounds were obtained in excellent overall yields and will be further used for determining the conformation of an alkyl chain of lipidic biomolecules upon interaction with proteins.
- Lethu, Sebastien,Matsuoka, Shigeru,Murata, Michio
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supporting information
p. 844 - 847
(2014/03/21)
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- Novel Antitumor Agents CI-920, PD 113270 and PD 113271. 3. Structure Determination.
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The chemical structures for the novel phosphate-containing antitumor agents CI-920 (1), PD 113270 (2), and PD 113271 (3) were determined by a combination of spectra and chemical means.Extensive analysis of NMR spectral data allowed tentative structures to be assigned for these compounds and their derivatives.These structures were confirmed by reducing CI-920 to 8-methyl-1-octadecanol and by cleaving dephosphorylated CI-920 (7) with sodium periodate to identified products.
- Hokanson, Gerard C.,French, James C.
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p. 462 - 466
(2007/10/02)
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