Datensatz

Zusammenfassung

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.