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

ABSTRACT: An improved method for the synthesis of 17?-hydroxy-16?-iodo-wortmannin along with the first synthesis of 17?-hydroxy-16?-iodoPX866 and [(131)I] radiolabeled 17?-hydroxy-16?-[(131)I]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.

SUBMITTER: Sun D

PROVIDER: S-EPMC3960976 | biostudies-literature | 2013 Sep

REPOSITORIES: biostudies-literature

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

Sun Duoli D Bhanu Prasad Basvoju A BA Schuber Paul T PT Peng Zhenghong Z Maxwell David S DS Martin Diana V DV Guo Liwei L Han Dongmei D Kurihara Hiroaki H Yang David J DJ Gelovani Juri G JG Powis Garth G Bornmann William G WG

Bioorganic & medicinal chemistry 20130627 17

An improved method for the synthesis of 17β-hydroxy-16α-iodo-wortmannin along with the first synthesis of 17β-hydroxy-16α-iodoPX866 and [(131)I] radiolabeled 17β-hydroxy-16α-[(131)I]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. ...[more]

PMID: 23859776

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