Convenient direct NCA electrophilic radioiodination of arenes using Iodo-gen™

Krummeich, C.; Holschbach, M.; Stöcklin, G.

doi:10.1016/0969-8043(96)00013-9

Cited by 8 publications

(2 citation statements)

References 16 publications

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“…The radiolabeled polymer was separated from noncovalently attached iodine on a Sephadex G-25 column. Compound III containing the methoxyphenol group was not readily radiolabeled when using the chloramines T reaction described in ref 37 but was readily radioiodinated using noncarrier iodine and an electrophilic protocol based upon Krummeich et al (38). In brief, 3 mg of III was dissolved in 0.25 mL of trifluoroacetic acid (TFA), and 0.01 mL of an aqueous solution of 125 I was added containing 1 mCi 125 I. Chloramine T (0.54 mg) dissolved in 0.05 mL of TFA was added to the mixture, and the reaction was heated at 60°C for 5 min.…”

Section: Methodsmentioning

confidence: 99%

Polyester Dendritic Systems for Drug Delivery Applications: In Vitro and In Vivo Evaluation

et al. 2002

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High molecular weight polymers (> 20 000 Da) have been widely used as soluble drug carriers to improve drug targeting and therapeutic efficacy. Dendritic polymers are exceptional candidates for the preparation of near monodisperse drug carriers due to their well-defined structure, multivalency, and flexibility for tailored functionalization. We evaluated various dendritic architectures composed of a polyester dendritic scaffold based on the monomer unit 2,2-bis(hydroxymethyl)propanoic acid for their suitability as drug carriers both in vitro and in vivo. These systems are both water soluble and nontoxic. In addition, the potent anticancer drug, doxorubicin, was covalently bound via a hydrazone linkage to a high molecular weight 3-arm poly(ethylene oxide)-dendrimer hybrid. Drug release was a function of pH, and the release rate was more rapid at pH < 6. The cytotoxicity of the DOX-polymer conjugate measured on multiple cancer lines in vitro was reduced but not eliminated, indicating that some active doxorubicin was released from the drug polymer conjugate under physiological conditions. Furthermore, biodistribution experiments show little accumulation of the DOX-polymer conjugate in vital organs, and the serum half-life of doxorubicin attached to an appropriate high molecular weight polymer has been significantly increased when compared to the free drug. Thus, this new macromolecular system exhibits promising characteristics for the development of new polymeric drug carriers.

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Section: Methodsmentioning

confidence: 99%

Polyester Dendritic Systems for Drug Delivery Applications: In Vitro and In Vivo Evaluation

et al. 2002

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“…Correspondingly, trifluoroacetyl hypoiodite was postulated as iodination agent for the n.c.a. radioiodination of tyrosine analogues and various anisole derivatives using Iodogen™ in TFA [31,32]. Finally the in situ formation of trifluoroacetyl hypoiodite is supported by the fact, that the reaction of N-iodosuccinimide in trifluoromethanesulfonic acid also leads to an intermediately formed iodo(I) trifluoromethanesulfonate (triflyl hypoiodite) as highly activated iodination species [33,34].…”

Section: Iodinating Speciesmentioning

confidence: 90%

Direct n.c.a. radioiodination of weakly activated arenes using metal salts

Mennicke¹,

Holschbach²,

Coenen

2000

Radiochimica Acta

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A new and simple synthesis of N‐succinimidyl‐4‐[^127/125I]iodobenzoate involving a microwave ‐ accelerated iodination step

Khalaj¹,

Beiki²,

Rafiee³

et al. 2001

Labelled Comp Radiopharmac

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A short and simple method for the preparation of N‐succinimidyl‐4‐iodobenzoate 3 and its 125I analogue that is widely used for radioiodination of proteins is described. The method involves the reaction of in situ generated trimethylsilyl iodide [127I or 125I] from trimethylsilyl chloride with N‐succinimidyl‐4‐[3,3‐(1,4‐butanediyl)‐triazene] benzoate 2 available from the condensation of N‐hydroxysuccinimide and 1‐(4‐carboxyphenyl)‐3,3‐(1,4‐butanediyl)‐triazene 1 in the presence of dicyclohexyl carbodiimide (DCC). The new triazene 1 was prepared by precipitating the diazonium ion of 4‐aminobenzoic acid with pyrrolidine. A microwave‐mediated rate acceleration was observed during the iodination step and by applying this procedure the labelled compound 3 was obtained in 81% radiochemical yield in 8 minutes. Copyright © 2001 John Wiley & Sons, Ltd.

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Convenient direct NCA electrophilic radioiodination of arenes using Iodo-gen™

Cited by 8 publications

References 16 publications

Polyester Dendritic Systems for Drug Delivery Applications: In Vitro and In Vivo Evaluation

Polyester Dendritic Systems for Drug Delivery Applications: In Vitro and In Vivo Evaluation

Direct n.c.a. radioiodination of weakly activated arenes using metal salts

A new and simple synthesis of N‐succinimidyl‐4‐[^127/125I]iodobenzoate involving a microwave ‐ accelerated iodination step

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Convenient direct NCA electrophilic radioiodination of arenes using Iodo-gen™

Cited by 8 publications

References 16 publications

Polyester Dendritic Systems for Drug Delivery Applications: In Vitro and In Vivo Evaluation

Polyester Dendritic Systems for Drug Delivery Applications: In Vitro and In Vivo Evaluation

Direct n.c.a. radioiodination of weakly activated arenes using metal salts

A new and simple synthesis of N‐succinimidyl‐4‐[127/125I]iodobenzoate involving a microwave ‐ accelerated iodination step

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A new and simple synthesis of N‐succinimidyl‐4‐[^127/125I]iodobenzoate involving a microwave ‐ accelerated iodination step