Synthesis and radiolabelling of Re(CO)<sub>3</sub>‐<i>β</i>‐elemene derivatives as potential therapeutic radiopharmaceuticals

Ren, Yunfeng; Sun, Yanhong; Cheng, Kangmin; Shen, Yu‐Mei

doi:10.1002/jlcr.1580

Cited by 6 publications

References 21 publications

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A facile automated synthesis of N‐succinimidyl 4‐[¹⁸F]fluorobenzoate ([¹⁸F]SFB) for ¹⁸F‐labeled cell‐penetrating peptide as PET tracer

Tang

Wang

2010

Labelled Comp Radiopharmac

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A fully automated synthesis of N‐succinimidyl 4‐[18F]fluorobenzoate ([18F]SFB) was carried out by a convenient three‐step, one‐pot procedure on the modified TRACERlab FXFN synthesizer, including [18F]fluorination of ethyl 4‐(trimethylammonium triflate)benzoate as the precursor, saponification of the ethyl 4‐[18F]fluorobenzoate with aqueous tetrapropylammonium hydroxide instead of sodium hydroxide, and conversion of 4‐[18F]fluorobenzoate salt ([18F]FBA) to [18F]SFB treated with N,N,N′,N′‐tetramethyl‐O‐(N‐succinimidyl)uranium tetrafluoroborate (TSTU). The purified [18F]SFB was used for the labeling of Tat membrane‐penetrating peptide (containing the Arg‐Lys‐Lys‐Arg‐Arg‐Arg‐Arg‐Arg‐Arg‐Arg‐Arg‐Pro‐Leu‐Gly‐Leu‐Ala‐Gly‐Glu‐Glu‐Glu‐Glu‐Glu‐Glu‐Glu sequence, [18F]CPP) through radiofluorination of lysine amino groups. The uncorrected radiochemical yields of [18F]SFB were as high as 25–35% (based on [18F]fluoride) (n=10) with a synthesis time of∼40 min. [18F]CPP was produced in an uncorrected radiochemical yields of 10–20% (n=5) within 30 min (based on [18F]SFB). The radiochemical purities of [18F]SFB and [18F]CPP were greater than 95%. Copyright © 2010 John Wiley & Sons, Ltd.

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A facile automated synthesis of N‐succinimidyl 4‐[¹⁸F]fluorobenzoate ([¹⁸F]SFB) for ¹⁸F‐labeled cell‐penetrating peptide as PET tracer

Tang

Wang

2010

Labelled Comp Radiopharmac

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Synthesis, characterization, and in vitro antiproliferative activity of novel β-elemene monosubstituted derivatives

Kong

Shen

2013

Med Chem Res

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Radioactive synthesis and biodistribution study of β-elemene–99mTc(CO)3 conjugates

et al. 2009

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Beta-elemene, (5S,7R,10S)-(-)-(1-methyl-1-vinyl-2,4-diisopropenylcyclohexane), is an anticancer agent from traditional Chinese herbal medicine. Three novel (99m)Tc(CO)(3)-beta-elemene conjugates were synthesized successfully, and compared with beta-elemene exhibited improved water solubility. A biodistribution and micro single photon emission computed tomography image study showed there is a visible accumulation in Lewis lung cancer tumors.

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Synthesis and radiolabelling of Re(CO)₃‐β‐elemene derivatives as potential therapeutic radiopharmaceuticals

Cited by 6 publications

References 21 publications

A facile automated synthesis of N‐succinimidyl 4‐[¹⁸F]fluorobenzoate ([¹⁸F]SFB) for ¹⁸F‐labeled cell‐penetrating peptide as PET tracer

A facile automated synthesis of N‐succinimidyl 4‐[¹⁸F]fluorobenzoate ([¹⁸F]SFB) for ¹⁸F‐labeled cell‐penetrating peptide as PET tracer

Synthesis, characterization, and in vitro antiproliferative activity of novel β-elemene monosubstituted derivatives

Radioactive synthesis and biodistribution study of β-elemene–99mTc(CO)3 conjugates

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Synthesis and radiolabelling of Re(CO)3‐β‐elemene derivatives as potential therapeutic radiopharmaceuticals

Cited by 6 publications

References 21 publications

A facile automated synthesis of N‐succinimidyl 4‐[18F]fluorobenzoate ([18F]SFB) for 18F‐labeled cell‐penetrating peptide as PET tracer

A facile automated synthesis of N‐succinimidyl 4‐[18F]fluorobenzoate ([18F]SFB) for 18F‐labeled cell‐penetrating peptide as PET tracer

Synthesis, characterization, and in vitro antiproliferative activity of novel β-elemene monosubstituted derivatives

Radioactive synthesis and biodistribution study of β-elemene–99mTc(CO)3 conjugates

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Synthesis and radiolabelling of Re(CO)₃‐β‐elemene derivatives as potential therapeutic radiopharmaceuticals

A facile automated synthesis of N‐succinimidyl 4‐[¹⁸F]fluorobenzoate ([¹⁸F]SFB) for ¹⁸F‐labeled cell‐penetrating peptide as PET tracer

A facile automated synthesis of N‐succinimidyl 4‐[¹⁸F]fluorobenzoate ([¹⁸F]SFB) for ¹⁸F‐labeled cell‐penetrating peptide as PET tracer