Synthesis and biodistribution of 99mTc-peptides conjugated adenine as tumor imaging agents

Zhao, Yanyu; Zhang, C. L.; Qi, Chunjian; Feng, Shiyu; You, Guangjiao; Fu, Zhanli; Guo, Fengqing; Wang, R. F.

doi:10.1007/s10967-007-0702-3

Cited by 3 publications

(2 citation statements)

References 6 publications

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“…Surprisingly, the clearance of diastereomers 99m Tc-11A and 11B occurred also via the hepatobiliary pathway despite of their negative charge. Polar compounds bearing a negative charge are considered to be hydrophilic in nature and expected to clear more via the renal pathway [30].…”

Section: In Vivo Studiesmentioning

confidence: 99%

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Development and biological evaluation of 99mTc-sulfonamide derivatives for in vivo visualization of CA IX as surrogate tumor hypoxia markers

Akurathi

Dubois

Celen

et al. 2014

European Journal of Medicinal Chemistry

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In vivo visualization of tumor hypoxia related markers, such as the endogenous transmembrane protein CA IX may lead to novel therapeutic and diagnostic applications in the management of solid tumors. In this study 4-(2-aminoethyl)benzene sulfonamide (AEBS, K(i) = 33 nM for CA IX) has been conjugated with bis(aminoethanethiol) (BAT) and mercaptoacetyldiglycine (MAG2) tetradendate ligands and the conjugates radiolabelled with (99m)Tc, to obtain anionic and neutral (99m)Tc-labeled sulfonamide derivatives, respectively. The corresponding rhenium analogues were also prepared and showed good inhibitory activities against hCA IX (K(i) = 59-66 nM). In addition, a second generation bis AEBS was conjugated with MAG2 and labeled with (99m)Tc, and the obtained diastereomers were also evaluated in targeting CA IX. Biodistribution studies in mice bearing HT-29 colorectal xenografts revealed a maximum tumor uptake of <0.5% ID/g at 0.5 h p.i for all the tracers. In vivo radiometabolite analysis indicated that at 1 h p.i. MAG₂ tetradendate ligands were more stable in plasma (>50% intact) compared to the neutral complex (28% intact). This preliminary data suggest that negatively charged (99m)Tc-labeled sulfonamide derivatives with modest lipophilicity and longer circulation time could be promising markers to target CA IX.

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Section: In Vivo Studiesmentioning

confidence: 99%

“…The conjugation reaction was performed using similar reaction conditions as reported by Zhao et al [30]. To a solution of 4-(2aminoethyl)benzenesulfonamide (1.54 mmol, 308 mg) in 5 mL DMF, Bn-MAG 2 (1.54 mmol, 453 mg), DMAP (3.08 mmol, 375 mg) and PyBOP (3.08 mmol, 1.56 g) were added.…”

Section: Conjugation Of Aebs With S-benzyl-mag 2 (5)mentioning

confidence: 99%

Development and biological evaluation of 99mTc-sulfonamide derivatives for in vivo visualization of CA IX as surrogate tumor hypoxia markers

Akurathi

Dubois

Celen

et al. 2014

European Journal of Medicinal Chemistry

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(S)-2-((S)-2-(4-(3-[18F]fluoropropyl)benzamido)-3-phenylpropanamido)pentanedioic acid labeled with 18F

Ding

Liu

et al. 2010

J Radioanal Nucl Chem

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Radiochemistry

Urch

2008

Annu. Rep. Prog. Chem., Sect. A: Inorg. Chem.

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This year's report on recent progress in Radiochemistry considers radiochemical methods in isotope production, advances in labelling procedures, radioactive isotopes in the environment and miscellaneous topics of radiochemical interest. Radiation chemistry, neutron activation analysis and the chemistry of elements that happen to be radioactive will be eschewed. HighlightsThe labelling of glucose 91 with oxygen-15!-from cyclotron to product in just seven minutes. A solution to part of nuclear waste problem by transmutation of technetium 381 into a stable ruthenium isotope. And the possibility of varying 46 radioactive half-lives by chemical means-to be confirmed.

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Synthesis and biodistribution of 99mTc-peptides conjugated adenine as tumor imaging agents

Cited by 3 publications

References 6 publications

Development and biological evaluation of 99mTc-sulfonamide derivatives for in vivo visualization of CA IX as surrogate tumor hypoxia markers

Development and biological evaluation of 99mTc-sulfonamide derivatives for in vivo visualization of CA IX as surrogate tumor hypoxia markers

(S)-2-((S)-2-(4-(3-[18F]fluoropropyl)benzamido)-3-phenylpropanamido)pentanedioic acid labeled with 18F

Radiochemistry

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