𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis and in vitro evaluation of 2-[11C]methoxyestradiol-3,17β-O,O-bissulfamate for in vivo studies of angiogenesis

✍ Scribed by Choong Mo Kang; Yearn Seong Choe; Kyung-Ho Jung; Joon Young Choi; Kyung-Han Lee; Byung-Tae Kim

Publisher
John Wiley and Sons
Year
2011
Tongue
French
Weight
339 KB
Volume
54
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

In the present study, 2‐methoxyestradiol‐3,17β‐O,O‐bissulfamate (1), a known angiogenesis inhibitor, was prepared in a radiolabeled form by ^11^C‐methylation of 2‐hydroxyestradiol‐3,17β‐O,O‐bis(N‐trityl)sulfamate (6) followed by detritylation. Synthesis of precursor 6 required a rather long step because of the presence of two sulfamoyl groups. The decay‐corrected radiochemical yield of [^11^C]1 was 19 ± 2% based on [^11^C]CH~3~I, and the specific activity was 34–39 GBq/µmol. Although 1 is known to significantly inhibit the proliferation of human umbilical vascular endothelial cells (HUVECs), its radiolabeled form, [^11^C]1 was not avidly taken up by HUVECs, and the uptake increased slightly in a time‐dependent manner (156% at 60 min relative to a value of 100% at 5 min). These results suggest that further studies are warranted to determine the molecular target for [^11^C]1. Copyright © 2011 John Wiley & Sons, Ltd.

📜 SIMILAR VOLUMES

Synthesis of a radiotracer for studying
Synthesis of a radiotracer for studying dopamine uptake sites in vivo using PET: 2β-carbomethoxy-3β-(4-fluorophenyl)-[N-11C-methyl]tropane ([11C]CFT or [11C]WIN-35,428)
✍ Robert F. Dannals; John L. Neumeyer; Richard A. Milius; Hayden T. Ravert; Alan A 📂 Article 📅 1993 🏛 John Wiley and Sons 🌐 French ⚖ 320 KB

## Abstract 2β‐Carbomethoxy‐3β‐(4‐fluorophenyl)‐[N‐^11^C‐methyl]tropane, a potent inhibitor of dopamine transport, was prepared by N‐methylation of the appropriate nor‐methyl precursor in DMF with [^11^C]iodomethane. After derivatization of unreacted precursor with a long chain acyl halide, the rad

Synthesis and in vivo evaluation of [O-m
Synthesis and in vivo evaluation of [O-methyl-11C] 2-(4-methoxyphenyl)-N-(4-methylbenzyl)-N-(1-methyl- piperidin-4-yl)acetamide as an imaging probe for 5-HT2A receptors
✍ Jaya Prabhakaran; Ramin V. Parsey; Vattoly J. Majo; Ronald L. Van Heertum; J. Jo 📂 Article 📅 2006 🏛 John Wiley and Sons 🌐 French ⚖ 224 KB 👁 1 views

## Abstract 2‐(4‐Methoxyphenyl)‐__N__‐(4‐methylbenzyl)‐__N__‐(1‐methylpiperidin‐4‐yl)acetamide (AC90179, **4**), a highly potent and selective competitive 5‐HT~2A~ antagonist, was labeled by [^11^C]‐methylation of the corresponding desmethyl analogue **5** with [^11^C]methyl triflate. The precursor