Improved synthesis of 17β-hydroxy-16α-iodo-wortmannin, 17β-hydroxy-16α-iodoPX866, and the [131I] analogue as useful PET tracers for PI3-kinase

An improved method for the synthesis of 17β-hydroxy-16α-iodo-wortmannin along with the first synthesis of 17β-hydroxy-16α-iodoPX866 and [131I] radiolabeled 17β-hydroxy-16α-[131I]iodo-wortmannin, as potential PET tracers for PI3K was also described. The differences between wortmannin and its iodo ana...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2013-09, Vol.21 (17), p.5182-5187
Hauptverfasser:	Sun, Duoli, Bhanu Prasad, Basvoju A., Schuber, Paul T., Peng, Zhenghong, Maxwell, David S., Martin, Diana V., Guo, Liwei, Han, Dongmei, Kurihara, Hiroaki, Yang, David J., Gelovani, Juri G., Powis, Garth, Bornmann, William G.
Format:	Artikel
Sprache:	eng
Schlagworte:	17β-Hydroxy-16α-[131I]iodowortmannin 17β-Hydroxy-16α-iodoPX866 17β-Hydroxy-16α-iodowortmannin Androstadienes - chemical synthesis Androstadienes - chemistry Binding Sites chemistry Gonanes - chemical synthesis Gonanes - chemistry Iodine Radioisotopes - chemistry Isotope Labeling Molecular Docking Simulation phosphatidylinositol 3-kinase Phosphatidylinositol 3-Kinase - chemistry Phosphatidylinositol 3-Kinase - metabolism PI3 kinase Positron emission tomography (PET) imaging Positron-Emission Tomography Protein Structure, Tertiary radiolabeling Radiopharmaceuticals - chemical synthesis Radiopharmaceuticals - chemistry Wortmannin
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Zusammenfassung:	An improved method for the synthesis of 17β-hydroxy-16α-iodo-wortmannin along with the first synthesis of 17β-hydroxy-16α-iodoPX866 and [131I] radiolabeled 17β-hydroxy-16α-[131I]iodo-wortmannin, as potential PET tracers for PI3K was also described. The differences between wortmannin and its iodo analogue were compared by covalently docking each structure to L833 in PI3K. An improved method for the synthesis of 17β-hydroxy-16α-iodo-wortmannin along with the first synthesis of 17β-hydroxy-16α-iodoPX866 and [131I] radiolabeled 17β-hydroxy-16α-[131I]iodo-wortmannin, as potential PET tracers for PI3K was also described. The differences between wortmannin and its iodo analogue were compared by covalently docking each structure to L833 in PI3K.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2013.06.036