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

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.

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 Creators:
Gerdes, Jantje Mareike1, Author
Waldmann, Herbert1, Referee           
Affiliations:
1Abt. IV: Chemische Biologie, Max Planck Institute of Molecular Physiology, Max Planck Society, Otto-Hahn-Str. 11, 44227 Dortmund, DE, ou_1753290              

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Free keywords: Festphasensynthese; Massenspektrometrie; Signaltransduktion. Guanosintriphosphatasen ; Enzymaktivator ; Chemische Synthese ; Festphasentechnik ; Reaktionsmechanismus ; MALDI-TOF-Massenspektrometrie
 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.

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Language(s): deu - German
 Dates: 2003-05-22
 Publication Status: Accepted / In Press
 Pages: pp. 161
 Publishing info: Dortmund : Universität Dortmund
 Table of Contents: -
 Rev. Type: -
 Degree: PhD

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