283173-74-0Relevant academic research and scientific papers
Copper-Mediated Radiosynthesis of [18F]Rucaparib
Chen, Zijun,Destro, Gianluca,Guibbal, Florian,Chan, Chung Ying,Cornelissen, Bart,Gouverneur, Véronique
, p. 7290 - 7294 (2021/09/14)
The poly(ADP-ribose) polymerase (PARP) inhibitor rucaparib is used in the clinic to treat BRCA-mutated cancers. Herein, we report two strategies to access the 18F-isotopologue of rucaparib by applying a copper-mediated nucleophilic 18F-fluorodeboronation. The most successful approach features an aldehydic boronic ester precursor that is subjected to reductive amination post-18F-labeling and affords [18F]rucaparib with an activity yield of 11% ± 3% (n = 3) and a molar activity (Am) up to 30 GBq/μmol. Preliminary in vitro studies are presented.
Poly(ADP-ribose) Polymerase in Neurodegeneration: Radiosynthesis and Radioligand Binding in ARC-SWE tg Mice
Alluri, Santosh R.,Riss, Patrick J.
, p. 1259 - 1263 (2018/06/26)
We report the synthesis, radiosynthesis, and characterization of a radioligand for poly(ADP-ribose) polymerase (PARP). PARP is of central importance in cell homeostasis, neuroplasticity, and neurodegeneration in the brain. A radiolabeled PARP inhibitor was developed and used for autoradiographic quantification of PARP protein concentration in wild-type and transgenic rodent brains ex vivo in high resolution. The binding of [3H]rucaparib was found to be confined to PARP-expressing domains, for example, cerebellar cortex or hippocampal regions in both models. Saturation binding experiments confirmed selective and reversible binding to a single site (Kd = 1.1 ± 0.2 nM).
Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis, and X-ray cocrystal structure
Canan Koch, Stacie S.,Thoresen, Lars H.,Tikhe, Jayashree G.,Maegley, Karen A.,Almassy, Robert J.,Li, Jianke,Yu, Xiao-Hong,Zook, Scott E.,Kumpf, Robert A.,Zhang, Cathy,Boritzki, Theodore J.,Mansour, Rena N.,Zhang, Kanyin E.,Ekker, Anne,Calabrese, Chris R.,Curtin, Nicola J.,Kyle, Suzanne,Thomas, Huw D.,Wang, Lan-Zhen,Calvert, A. Hilary,Golding, Bernard T.,Griffin, Roger J.,Newell, David R.,Webber, Stephen E.,Hostomsky, Zdenek
, p. 4961 - 4974 (2007/10/03)
A series of novel compounds have been designed that are potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1), and the activity and physical properties have been characterized. The new structural classes, 3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol
