Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells

Nifurtimox reduces N-Myc expression and aerobic glycolysis in neuroblastoma

“…In contrary cytotoxic effects were far less in SK-N-SH compared to the MYCN amplified cell lines. [43][44][45][46][47] These analyses substantiate the hypothesis that N-Myc is related to glycolysis.…”

1-(N,N-Dialkylcarbamoyl)-1,1-difluoromethanesulfonyl ester as a stable and effective precursor for a neopentyl labeling group with astatine-211

“…Therefore, we hypothesized that a base might improve the nucleophilicity of the astatine-containing chemical species. Therefore, we investigated labeling in the presence of K 2 CO 3 , which has a proven track record in the synthesis of 18 F-labeled compounds. As a result, the RCC value of neopentyl [ 211 At]astatide 4d in the reaction with the residue containing 211 At with CDf ester 3A (2.5 µmol) and K 2 CO 3 (0.5 mg) in acetonitrile (35 µL) at 70 °C for 10 min was 95%.…”

“…The neopentyl labeling group present in 1 has recently been identified as an effective hydrophilic labeling unit for various radiohalogens, which includes both 18 F and 211 At (Scheme 1). [4][5][6] The carbon-halogen bond in the labeling group exhibits high in vivo stability and significantly resists dehalogenation even in 211 At-labeled compounds.…”

Nuclear Medicine Imaging in Neuroblastoma: Current Status and New Developments

“…18 F-labeled fluoropropylbenzylguanidine (FPBG) PET-CT detected one extra (histologically confirmed) metastatic bone lesion compared to [ 123 I]mIBG scintigraphy in a case report of a neuroblastoma patient [ 113 ]. Other analogues that have only been studied in neuroblastoma cell lines are parafluorobenzylguanidine (PFBG) [ 114 ], LMI1195 (N-[3-bromo-4-(3-F-fluoro-propoxy)-benzyl]-guanidine) [ 115 ], FPOIBG (4-fluoropropoxy-3-iodobenzylguanidine) [ 116 ], and meta -bromobenzylguanidine (mBBG) [ 117 ].…”

“…18 F-labeled fluoropropylbenzylguanidine (FPBG) PET-CT detected one extra (histologically confirmed) metastatic bone lesion compared to [ 123 I]mIBG scintigraphy in a case report of a neuroblastoma patient [113]. Other analogues that have only been studied in neuroblastoma cell lines are parafluorobenzylguanidine (PFBG) [114], LMI1195 (N-[3-bromo-4-(3-F-fluoro-propoxy)-benzyl]-guanidine) [115], FPOIBG (4-fluoropropoxy-3iodobenzylguanidine) [116], and meta-bromobenzylguanidine (mBBG) [117]. [118]; an antagonist of CXC chemokine receptor 4 (CXCR4), frequently overexpressed in various tumor types in the form of 68 Ga-labeled pentixafor and 177 Lulabeled pentixather [119]; and zirconium-89 ( 89 Zr)-labeled dinutuximab, a radiolabeled anti-GD2 immunotherapy [120].…”