de.mpg.escidoc.pubman.appbase.FacesBean
English
 
Help Guide Disclaimer Contact us Login
  Advanced SearchBrowse

Item

ITEM ACTIONSEXPORT

Released

Thesis

Strategien zum Aufbau niedermolekularer GTPase-Aktivatoren und zur direkten massenspektrometrischen Reaktionskontrolle am polymeren Träger (MS-SPOS)

MPS-Authors

Gerdes,  Jantje Mareike
Abt. IV: Chemische Biologie, Max Planck Institute of Molecular Physiology, Max Planck Society;

http://pubman.mpdl.mpg.de/cone/persons/resource/persons98735

Waldmann,  Herbert
Abt. IV: Chemische Biologie, Max Planck Institute of Molecular Physiology, Max Planck Society;

Locator
There are no locators available
Fulltext (public)
There are no public fulltexts available
Supplementary Material (public)
There is no public supplementary material available
Citation

Gerdes, J. M. (2003). Strategien zum Aufbau niedermolekularer GTPase-Aktivatoren und zur direkten massenspektrometrischen Reaktionskontrolle am polymeren Träger (MS-SPOS). PhD Thesis, Universität Dortmund, Dortmund.


Cite as: http://hdl.handle.net/11858/00-001M-0000-0014-0C84-3
Abstract
Solid phase synthesis of potential small molecule GTPase activators was carried out on both Wang PS and PEGA resin. Benzophenone substructures were assemlbed using a sequential iodine-mgnesium bromide exchange reaction followed by transmetallation and acylation by an activated organic acid. Both 3-aminobenzoyl, 6-aminonicotinoyl, and aminothiazole groups were synthesized. The aminothizole derivatives proved to inhibit receptor tyrosine kinases in the low micromolecular range [IC50]. Direct on-bead monitoring of solid phase reactions is possible with MALDI-TOF MS under matrix-free conditions and without prior cleavage from the resin if photocleavable phenacyl ester or o-nitroveratryl linker groups are employed.