N. C. A. radioiodination of idoxifene

Trivedi, Mahendra; POTTER, G. F.; Hammersley, P. A. G.; Carnochan, P.; Young, Helen; Jarman, Michael; Ott, R. J.

doi:10.1002/jlcr.2580361003

Cited by 5 publications

(4 citation statements)

References 6 publications

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“…Purification of 131 I‐ 5p was achieved via preparative thin‐layer silica gel plates [ 47,48 ] using chloroform: methanol (4.8:0.2 vol/vol) as eluent. The band for the cold precursor ( 5p ) was detected using UV‐lamp (254 nm) [ 47 ] at R f = 0.50 while the free radioiodine remained at the base. The band corresponding to 131 I‐ 5p ( R f = 0.55) was scrapped and vortexed for 1 min with benzene (1 mL × 2).…”

Section: Methodsmentioning

confidence: 99%

“…Purification of 131 I-5p was achieved via preparative thin-layer silica gel plates [47,48] using chloroform: methanol (4.8:0.2 vol/vol) as eluent.…”

Section: Purification Of 131 I-5pmentioning

confidence: 99%

“…The band for the cold precursor (5p) was detected using UV-lamp (254 nm) [47] at R f = 0.50 while the free radioiodine remained at the base. The band corresponding to 131 I-5p (R f = 0.55) was scrapped and vortexed for 1 min with benzene (1 mL × 2).…”

Section: Purification Of 131 I-5pmentioning

confidence: 99%

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Novel substituted 1,8‐naphthyridines: Design, synthesis, radiolabeling, and evaluation of apoptosis and topoisomerase II inhibition

Abuzahra

Ahmed

Sarhan

et al. 2023

Archiv der Pharmazie

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A series of seventeen 1,8-naphthyridine derivatives (5a-5q) conjugated at N 1 to various substituted phenyl rings were designed and synthesized as potential topoisomerase II (Topo II) inhibitors. The antiproliferative activity of the target compounds against three cancer cell lines showed that compounds 5g and 5p had the highest antiproliferative activity. In addition, 5p and 5g displayed a high selectivity index (SI) for cancer cells when tested on WI38 normal cells, whereby compound 5p showed the highest SI. Furthermore, 5g and 5p induced cell cycle arrest at the S and G1/S phases, respectively, triggering apoptosis in HepG-2 cells.The in vitro Topo II inhibitory effect (plasmid-based) of both compounds revealed that 5p had better inhibition of Topo II. In addition, 5p displayed potent topoisomerase IIβ inhibitory effect when compared to known topoisomerase inhibitors (doxorubicin and topotecan). Molecular docking proposed a unique binding pattern of 5p in the etoposide binding pocket of topoisomerase IIβ, endorsing its potential role as a Topo II poison. Accordingly, 5p was chosen for radioiodination to study the degree of tumor localization following administration in solid tumor-bearing mice. The radioiodinated 5p showed a selective localization at the tumor site, which further confirmed the value of 5p as a lead 1,8-naphthyridine anticancer agent.

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Section: Methodsmentioning

confidence: 99%

“…Purification of 131 I-5p was achieved via preparative thin-layer silica gel plates [47,48] using chloroform: methanol (4.8:0.2 vol/vol) as eluent.…”

Section: Purification Of 131 I-5pmentioning

confidence: 99%

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Novel substituted 1,8‐naphthyridines: Design, synthesis, radiolabeling, and evaluation of apoptosis and topoisomerase II inhibition

Abuzahra

Ahmed

Sarhan

et al. 2023

Archiv der Pharmazie

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“…material of good radiochemical purity (95%) which may be further purified by HPLC with 70% recovery. 183 Iododestannylation was the essential step in the synthesis of [I-125]iodoproxyfan, the arylstannane being obtained through the Pd-catalysed coupling of hexabutylditin and the aryl bromide. Radio-iodine was generated from [I-125]-NaI and Chloramine-T.…”

Section: Iododemetallation and Halogen Exchangementioning

confidence: 99%

Radiohalogen incorporation into organic systems

Bolton

2002

Labelled Comp Radiopharmac

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SummaryThis Review reports the more recent applications of radiohalogen labelling in organic compounds. Modern synthetic methods place more emphasis upon substitution at specific sites. Electrophilic substitution, especially at aromatic carbon atoms, involves displacement of halogen or of metals rather than the earlier popular halogen-deprotiation processes. Nucleophilic displacement, at either aliphatic or aromatic sites, has also become widespread since it may be made more selective by the inclusion of appropriate activating groups or suitable displaced groups. Microwave and thermally induced methods are both reported with a critical assessment of the value of each process.

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Synthetic Applications of Organic Germanium, Tin and Lead Compounds (ExcludingR₃MH)

Fouquet

2009

Patai's Chemistry of Functional Groups

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N. C. A. radioiodination of idoxifene

Abstract: Summary: We describe a method for n.c.a. radioiodination of pyrrolidino tamoxifen (Idoxifene) based on the electrophilic destannylation of tributylstannyl pyrrolidino tamoxifen. The methods of separation using preparative tlc and HPLC give >95% radiochemical purity and > 7 0 % recovery.

Cited by 5 publications

References 6 publications

Novel substituted 1,8‐naphthyridines: Design, synthesis, radiolabeling, and evaluation of apoptosis and topoisomerase II inhibition

Novel substituted 1,8‐naphthyridines: Design, synthesis, radiolabeling, and evaluation of apoptosis and topoisomerase II inhibition

Radiohalogen incorporation into organic systems

Synthetic Applications of Organic Germanium, Tin and Lead Compounds (ExcludingR₃MH)

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N. C. A. radioiodination of idoxifene

Abstract: Summary: We describe a method for n.c.a. radioiodination of pyrrolidino tamoxifen (Idoxifene) based on the electrophilic destannylation of tributylstannyl pyrrolidino tamoxifen. The methods of separation using preparative tlc and HPLC give >95% radiochemical purity and > 7 0 % recovery.

Cited by 5 publications

References 6 publications

Novel substituted 1,8‐naphthyridines: Design, synthesis, radiolabeling, and evaluation of apoptosis and topoisomerase II inhibition

Novel substituted 1,8‐naphthyridines: Design, synthesis, radiolabeling, and evaluation of apoptosis and topoisomerase II inhibition

Radiohalogen incorporation into organic systems

Synthetic Applications of Organic Germanium, Tin and Lead Compounds (ExcludingR3MH)

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Product

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Synthetic Applications of Organic Germanium, Tin and Lead Compounds (ExcludingR₃MH)