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Titolo:
Fluoroazomycin arabinoside (FAZA): Synthesis, H-2 and H-3-labelling and preliminary biological evaluation of a novel 2-nitroimidazole marker of tissue hypoxia.
Autore:
Kumar, P; Stypinski, D; Xia, H; McEwan, AJB; Machulla, HJ; Wiebe, LI;
Indirizzi:
Univ Alberta, Dent Pharm Ctr 3118, Fac Pharm & Pharmaceut Sci, Noujaim Inst Univ Alberta Edmonton AB Canada T6G 2N8 rm & Pharmaceut Sci, Noujaim Inst Univ Alberta, Fac Med, Edmonton, AB T6G 2N8, Canada Univ Alberta EdmontonAB Canada T6G 2N8 Med, Edmonton, AB T6G 2N8, Canada Univ Tubingen Hosp, D-72076 Tubingen, Germany Univ Tubingen Hosp Tubingen Germany D-72076 p, D-72076 Tubingen, Germany
Titolo Testata:
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
fascicolo: 1, volume: 42, anno: 1999,
pagine: 3 - 16
SICI:
0362-4803(199901)42:1<3:FA(SHA>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
IMAGING TUMOR HYPOXIA; SOLID TUMORS; FLUOROMISONIDAZOLE; MISONIDAZOLE; ANGIOGENESIS; CELLS;
Keywords:
fluoroazomycin arabinoside; FAZA; IAZA; synthesis; deuteration; tritiation; radiosensitizer; hypoxia; tumour; pharmacokinetics; PET; SPECT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Physical, Chemical & Earth Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Wiebe, LI Univ Alberta, Dent Pharm Ctr 3118, Fac Pharm & Pharmaceut Sci, Noujaim Inst Univ Alberta Edmonton AB Canada T6G 2N8 aceut Sci, Noujaim Inst
Citazione:
P. Kumar et al., "Fluoroazomycin arabinoside (FAZA): Synthesis, H-2 and H-3-labelling and preliminary biological evaluation of a novel 2-nitroimidazole marker of tissue hypoxia.", J LABEL C R, 42(1), 1999, pp. 3-16

Abstract

1-alpha-D-(5-Fluoro-5-deoxyarabinofuranosyl)-2-nitroimidazole (fluoroazomycin arabinoside; FAZA), 6, a putative PET imaging agent when labelled with F-18, was synthesized by fluorination of 1-alpha-D-(2,3-di-O-acetylarabinofuranosyl)-2-nitroimidazole 3 with DAST followed by deprotection. The C-5'-deuterated and tritiated analogues were prepared by NaCNBD3 or NaCNBT3 reduction of the protected C-5'-carbonyl intermediate 5, followed by C-5' fluorination and deprotection, to afford C-5' deuterated and C-5' tritiated FAZA,respectively. Preliminary in vivo biodistribution studies in a murine tumour model, and pharmacokinetic studies in rats indicated that H-3-FAZA has biodistribution, tumour uptake and pharmacokinetic properties similar to those of I-123-IAZA, a clinically-proven radiopharamaceutical for SPECT-imaging of hypoxic tissues.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 18:34:08