title: Improved synthesis of 17β-hydroxy-16α-iodo-wortmannin, 17β-hydroxy-16α-iodoPX866, and the [(131)I] analogue as useful PET tracers for PI3-kinase.
abstract: 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.
authors.affiliation: Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, United States.
authors.forename: Duoli
authors.initials: D
authors.lastname: Sun
authors.forename: Basvoju A
authors.initials: BA
authors.lastname: Bhanu Prasad
authors.forename: Paul T
authors.initials: PT
authors.lastname: Schuber
authors.forename: Zhenghong
authors.initials: Z
authors.lastname: Peng
authors.forename: David S
authors.initials: DS
authors.lastname: Maxwell
authors.forename: Diana V
authors.initials: DV
authors.lastname: Martin
authors.forename: Liwei
authors.initials: L
authors.lastname: Guo
authors.forename: Dongmei
authors.initials: D
authors.lastname: Han
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Kurihara
authors.forename: David J
authors.initials: DJ
authors.lastname: Yang
authors.forename: Juri G
authors.initials: JG
authors.lastname: Gelovani
authors.forename: Garth
authors.initials: G
authors.lastname: Powis
authors.forename: William G
authors.initials: WG
authors.lastname: Bornmann
mesh_terms: D000730:Androstadienes / Q000138:chemical synthesis* / Q000737:chemistry*; D001665:Binding Sites; D006067:Gonanes / Q000138:chemical synthesis* / Q000737:chemistry; D007457:Iodine Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling; D062105:Molecular Docking Simulation; D058539:Phosphatidylinositol 3-Kinase / Q000737:chemistry / Q000378:metabolism; D049268:Positron-Emission Tomography; D017434:Protein Structure, Tertiary; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D000077191:Wortmannin
chemical_list: C586726:17beta-hydroxy-16alpha-iodo-wortmannin; C586728:17beta-hydroxy-16alpha-iodoPX866; D000730:Androstadienes; D006067:Gonanes; D007457:Iodine Radioisotopes; D019275:Radiopharmaceuticals; D058539:Phosphatidylinositol 3-Kinase; D000077191:Wortmannin
keywords: 17β-Hydroxy-16α-[(131)I]iodowortmannin; 17β-Hydroxy-16α-iodoPX866; 17β-Hydroxy-16α-iodowortmannin; LYDLNTRBZQFQTG-RUXBYQPCSA-N; OWEYHVVHIWKFGJ-TUYZGLGGSA-N; PI3 kinase; Positron emission tomography (PET) imaging