vorozole

Vorozole
Systematic (IUPAC) name
	6-[(4-Chlorophenyl)(1,2,4-triazol-1-yl)methyl]-1-methylbenzotriazole
Clinical data
Legal status	?
Pharmacokinetic data
Bioavailability	Very high
Metabolism	Hepatic
Half-life	8 hours
Identifiers
CAS number	118949-22-7
ATC code	L02BG05
PubChem	CID 6918191
ChemSpider	5293402
UNII	1E2S9YXV2A
KEGG	D03786
ChEMBL	CHEMBL224060
Chemical data
Formula	C16H13ClN6
Mol. mass	324.768 g/mol
	SMILES Clc1ccc(cc1)[C@@H](c2ccc3nnn(c3c2)C)n4ncnc4;
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/03/21 13:41:55」(JST)

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Vorozole is an imidazole based competitive inhibitor of the aromatase enzyme. It underwent clinical testing for evaluation for use as an antineoplastic agent; however it was withdrawn from testing when no difference was detected in the duration of median survival as compared to the progestational agent megestrol acetate and research instead focused on the other third generation aromatase inhibitors anastrozole, letrozole and exemestane.

It is selective.^[1]

Chemistry[edit]

Vorozole can be synthesized from 3-chloro-4-nitrobenzoic acid.^[2]

References[edit]

^ Goss PE (1998). "Pre-clinical and clinical review of vorozole, a new third generation aromatase inhibitor". Breast Cancer Res. Treat. 49. Suppl 1: S59–65; discussion S73–7. PMID 9797019.
^ Prous, J.; Grant, J.; Castaner, J.; Drugs Future 1994, 457.

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1. 転移性ホルモン受容体陽性乳癌に対する治療アプローチ：内分泌療法 treatment approach to metastatic hormone receptor positive breast cancer endocrine therapy

English Journal

Aromatase Imaging with [N-Methyl-11C]Vorozole PET in Healthy Men and Women.

Biegon A1, Alexoff DL2, Kim SW3, Logan J4, Pareto D5, Schlyer D2, Wang GJ3, Fowler JS6.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine.J Nucl Med.2015 Apr;56(4):580-5. doi: 10.2967/jnumed.114.150383. Epub 2015 Feb 19.
Aromatase, the last and obligatory enzyme catalyzing estrogen biosynthesis from androgenic precursors, can be labeled in vivo with (11)C-vorozole. Aromatase inhibitors are widely used in breast cancer and other endocrine conditions. The present study aimed to provide baseline information defining ar
PMID 25698781

Autoradiography screening of potential positron emission tomography tracers for asymptomatic abdominal aortic aneurysms.

Tegler G1, Estrada S, Hall H, Wanhainen A, Björck M, Sörensen J, Antoni G.
Upsala journal of medical sciences.Ups J Med Sci.2014 Aug;119(3):229-35. doi: 10.3109/03009734.2014.894157. Epub 2014 Feb 21.
OBJECTIVE: The aetiology and early pathophysiological mechanisms of aortic aneurysm formation are still unknown and challenging to study in vivo. Positron emission tomography (PET) is a potentially valuable instrument for non-invasive in vivo pathophysiological studies. No specific tracer to identif
PMID 24555564

11C-cetrozole: an improved C-11C-methylated PET probe for aromatase imaging in the brain.

Takahashi K1, Hosoya T, Onoe K, Doi H, Nagata H, Hiramatsu T, Li XL, Watanabe Y, Wada Y, Takashima T, Suzuki M, Onoe H, Watanabe Y.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine.J Nucl Med.2014 May;55(5):852-7. doi: 10.2967/jnumed.113.131474. Epub 2014 Mar 27.
Aromatase (an enzyme that converts androgens to estrogens) in the brain is involved in neuroprotection, synaptic plasticity, and regulation of sexual and emotional behaviors. To investigate the physiologic and pathologic importance of aromatase in the brain, including in humans, we here report the d
PMID 24676756

Japanese Journal

ラットDMBA誘発乳癌における新規aromatase阻害剤vorozoleの抗腫瘍効果とIGF-1抑制作用

菅又徳孝,飯野佑一,鯉淵幸生,安東立正,松本広志,前村道生,武井寛幸,堀口淳,横江隆夫,森下靖雄
日本外科学会雑誌 99(臨時増刊), 339, 1998-03-10
NAID 110003952557

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