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

Gerdes, Jantje Mareike

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

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

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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: https://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.