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001-es BibID:BIBFORM099499
035-os BibID:(WoS)000747265100001 (Scopus)85123424554
Első szerző:Csupász Tibor (1991-)
Cím:A New Oxygen Containing Pyclen-Type Ligand as a Manganese(II) Binder for MRI and 52Mn PET Applications: Equilibrium, Kinetic, Relaxometric, Structural and Radiochemical Studies / Tibor Csupász, Dániel Szücs, Ferenc Krisztián Kálmán, Oldamur Hollóczki, Anikó Fekete, Dezső Szikra, Éva Tóth, Imre Tóth, Gyula Tircsó
Dátum:2022
ISSN:1420-3049
Megjegyzések:A new pyclen-3,9-diacetate derivative ligand (H23,9-OPC2A) is synthesized possessing an etheric O-atom opposite to the pyridine ring, to improve the dissociation kinetics of its Mn(II) complex (pyclen = 3,6,9,15-tetraazabicyclo(9.3.1)pentadeca-1(15),11,13-triene). The new ligand is less basic than the N-containing analogue (H23,9-PC2A) due to the non-protonable O-atom. In spite of its lower basicity, the conditional stability of the (Mn(3,9-OPC2A)) (pMn = ?log(Mn(II)), cL = cMn(II) = 0.01 mM. pH = 7.4) remains unaffected (pMn = 8.69), compared to the (Mn(3,9-PC2A)) (pMn = 8.64). The (Mn(3,9-OPC2A)) possesses one water molecule, having a lower exchange rate with bulk solvents (kex298 = 5.3 ??0.4 ? 107 s?1) than (Mn(3,9-PC2A)) (kex298 = 1.26?108 s?1). These mild dif-ferences are rationalized by the density-functional theory (DFT) calculations. The acid assisted dissociation of (Mn(3,9-OPC2A)) is considerably slower (k1 = 2.81 ??0.07 M?1s?1) than that of the complexes of diacetates or bisamides of various 12-membered macrocycles and the parent H23,9-PC2A. The (Mn(3,9-OPC2A)) is inert in rat/human serum as confirmed by 52Mn labeling (nM range), as well as by relaxometry (mM range). However, a 600-fold excess of EDTA (pH = 7.4) or a mixture of essential metal ions, propagated some transchelation/transmetalation in 7 days. The H23,9-OPC2A is labeled efficiently with 52Mn at elevated temperatures, yet at 37 ?C the parent H23,9-PC2A performs slightly better. Ultimately, the H23,9-OPC2A shows advantageous features for further ligand designs for bifunctional chelators.
A new pyclen-3,9-diacetate derivative ligand (H23,9-OPC2A) is synthesized possessing an etheric O-atom opposite to the pyridine ring to improve the dissociation kinetics of its Mn(II) complex (pyclen = 3,6,9,15-tetraazabicyclo[9.3.1]pentadeca-1(15),11,13-triene). The new ligand is less basic than the N-containing analogue (H23,9-PC2A) due to the non-protonable O-atom. In spite of its lower basicity, the conditional stability of the [Mn(3,9-OPC2A)] (pMn=-log[Mn(II)], cL=cMn(II)=0.01 mM. pH=7.4) remains unaffected (pMn=8.69) compared to the [Mn(3,9-PC2A)] (pMn=8.64). The [Mn(3,9-OPC2A)] possesses one water molecule, having a lower exchange rate with bulk solvent (kex298=5.3?0.4?107 s-1) than [Mn(3,9-PC2A)] (kex298=1.26?108 s-1). These mild differences are ration-alized by density-functional theory (DFT) calculations. The acid assisted dissociation of [Mn(3,9-OPC2A)] is considerably slower (k1=2.81?0.07 M-1s-1) than that of the complexes of diac-etates or bisamides of various 12-membered macrocycles and the parent H23,9-PC2A. The [Mn(3,9-OPC2A)] is inert in rat/human serum as confirmed by 52Mn labeling (nM range) as well as by relaxometry (mM range). However, 600-fold excess of EDTA (pH=7.4) or a mixture of es-sential metal ions propagated some transchelation/transmetalation in 7 days. The H23,9-OPC2A is labeled efficiently with 52Mn at elevated temperatures, yet at 37 oC the parent H23,9-PC2A per-forms slightly better. Altogether the H23,9-OPC2A shows advantageous features for further lig-and design for bifunctional chelators.
Tárgyszavak:Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
Megjelenés:Molecules. - 27 (2022), p. 1-27. -
További szerzők:Szücs Dániel (1994-) (gyógyszerész) Kálmán Ferenc K. (1978-) (vegyész) Hollóczki Oldamur (1983-) (okleveles vegyészmérnök) Fekete Anikó (1973-) (vegyész) Szikra Dezső Péter (1983-) (vegyész) Tóth Éva Tóth Imre (1950-) (vegyész) Tircsó Gyula (1977-) (vegyész, kémia tanár)
Pályázati támogatás:K-120224
OTKA
K-128201
OTKA
K-134694
OTKA
FK-134551
OTKA
University of Debrecen Innovation Fund (POC-012)
Egyéb
the János Bolyai Research Scholarship of the Hungarian Academy of Sciences
MTA
ÚNKP-21-4 new national excellence program of the Ministry of Human Capacities
Egyéb
Doctoral School of Chemistry at the University of Debrecen
Egyéb
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001-es BibID:BIBFORM106173
035-os BibID:(cikkazonosító)122527 (scopus)85145300291 (WoS)000964725400001
Első szerző:Kálmán-Szabó Ibolya (molekuláris biológus)
Cím:61Cu-Labelled radiodiagnostics of melanoma with NAPamide-targeted radiopharmaceutical / Kálmán-Szabó Ibolya, Bunda Szilvia, Lihi Norbert, Szaniszló Zsófia, Szikra Dezső, Péliné Szabó Judit, Fekete Anikó, Gyuricza Barbara, Szücs Dániel, Papp Gábor, Trencsényi György, Kálmán Ferenc K.
Dátum:2023
ISSN:0378-5173
Megjegyzések:Malignant melanoma is a major public health problem with an increasing incidence and mortality in the Caucasian population due to its significant metastatic potential. The early detection of this cancer type by imaging techniques like positron emission tomography acts as an important contributor to the long-term survival. Based on literature data, the radio labelled alpha-MSH analog NAPamide molecule is an appropriate diagnostic tool for the detection of melanoma tumors. Inspired by these facts, a new radiotracer, the [61Cu]Cu-KFTG-NAPamide has been synthesized to exploit the beneficial features of the positron emitter 61Cu and the melanoma specificity of the NAPamide molecule. In this work, we report a new member of the CB-15aneN5 ligand family (KFTG) as the chelator for 61Cu(II) complexation. On the basis of the thorough physico-chemical characterization, the rigid [Cu(KFTG)]+ complex exhibits fast complex formation (t1/2=155 s at pH 5.0 and 25 ?C) and high inertness (t1/2=2.0 h in 5.0 M HCl at 50 ?C) as well as moderate superoxide dismutase activity (IC50=2.3 ?M). Furthermore, the [61Cu]Cu-KFTG-NAPamide possesses outstanding features in the diagnostics of B16-F10 melanoma tumors by PET imaging: (T/M(SUVs) (in vivo): appr. 14, %ID/g: 7?1 and T/M (ex vivo): 315?24 at 180 min).
Tárgyszavak:Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
Megjelenés:International Journal Of Pharmaceutics. - 632 (2023), p. 1-9. -
További szerzők:Bunda Szilvia (1992-) (vegyész) Lihi Norbert (1990-) (vegyész) Szaniszló Zsófia (1998-) (vegyészmérnök) Szikra Dezső Péter (1983-) (vegyész) Péli-Szabó Judit (1977-) (vegyész) Fekete Anikó (1973-) (vegyész) Gyuricza Barbara (1994-) (gyógyszerész) Szücs Dániel (1994-) (gyógyszerész) Papp Gábor (1976-) (vegyész, kémikus) Trencsényi György (1978-) (biológus, biokémikus, molekuláris biológus) Kálmán Ferenc K. (1978-) (vegyész)
Pályázati támogatás:FK-134551
Egyéb
ÚNKP-21-5
Egyéb
ÚNKP-22-5
Egyéb
Internet cím:Szerző által megadott URL
DOI
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