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Your search keyword '"Sheldrick, William S."' showing total 5 results
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5 results on '"Sheldrick, William S."'

2. Binuclear dioxomolybdenum(VI) complexes of some tridentate ONS donor ligand containing [MoO2]2+ as the acceptor center: Synthesis, crystal structure, supramolecular architectures via hydrogen bonds, π-π stacking and DFT calculations

Author

Pramanik, Nikhil Ranjan, Chakraborty, Manashi, Biswal, Debanjana, Mandal, Sudhanshu Sekhar, Ghosh, Saktiprosad, Chakrabarti, Syamal, Sheldrick, William S., Drew, Michael G.B., Mondal, Tapan Kumar, and Sarkar, Deblina

Published
2015
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5. The biological activity of Zeise's salt and its derivatives.

Author

Meieranz S, Stefanopoulou M, Rubner G, Bensdorf K, Kubutat D, Sheldrick WS, and Gust R

Subjects
Aspirin chemistry, Aspirin pharmacology, Cell Line, Tumor, Cell Proliferation drug effects, Cyclooxygenase Inhibitors chemical synthesis, Dose-Response Relationship, Drug, Enzyme Activation drug effects, Humans, MCF-7 Cells, Models, Molecular, Molecular Structure, Organoplatinum Compounds chemistry, Structure-Activity Relationship, Aspirin analogs & derivatives, Cyclooxygenase 1 metabolism, Cyclooxygenase Inhibitors chemistry, Cyclooxygenase Inhibitors pharmacology, Organoplatinum Compounds pharmacology, Salts chemistry
Abstract

With the aim to design new biologically active bioinorganic drugs of aspirin, whose mode of action is based on the inhibition of the cyclooxygenase(COX) enzymes, derivatives of Zeise's salt were synthesized in this structure-activity relationship study. Surprisingly, not only these Zeise-aspirin compounds but also Zeise's salt itself showed high inhibitory potency against COX enzymes in in vitro assays. In contrast, potassium tetrachloroplatinate and cisplatin did not influence the enzyme activity at equimolar concentrations. It was demonstrated by LC-ESI tandem-mass spectrometry that Zeise's salt platinates the essential amino acids Tyr385 (active site of the enzyme) and Ser516 (will be acetylated by aspirin) of COX-1, thereby strongly impairing the function of the enzyme. This finding demonstrates for the first time that Zeise's salt is pharmacologically active and is a potent enzyme inhibitor., (© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2015
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