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Synthesis, Design, And Biological Evaluation Of Inhibitors And Activators Of Src Homology 2 Domain-Containing Inositol Phosphatase (Ship) And Synthetic Studies Of Apicularen A And Maoecrystal V, Dennis Racca Viernes

Chemistry - Dissertations

This dissertation involves work both on the syntheses of small molecules with potential therapeutic applications and synthetic studies on natural products with unusual core skeletons.

The first part of this work involves the synthesis, design, and biological evaluation of aminosteroids as inhibitors for the SH2-containing inositol phosphatase 1 (SHIP1). SHIP1, a 145 kDa protein, is involved in regulating the formation of new blood cells. High- throughput screening identified several SHIP inhibitors including NSC23922, a mixture of 3a- and 3β-aminocholestane. Both 3a- and 3β-aminocholestane were synthesized from dihdyrocholesterol and the 3a- form was verified as …