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001-es BibID:	BIBFORM103610
035-os BibID:	(cikkazonosító)110978 (WOS)000522119300002 (Scopus)85077754827
Első szerző:	Guillou, Amaury
Cím:	Picolinate-appended tacn complexes for bimodal imaging: Radiolabeling, relaxivity, photophysical and electrochemical studies / Amaury Guillou, Margau Galland, Amandine Roux, Balázs Váradi, Réka Anna Gogolák, Patricia Le Saëc, Alain Faivre-Chauvet, Maryline Beyler, Christophe Bucher, Gyula Tircsó, Véronique Patinec, Olivier Maury, Raphaël Tripier
Dátum:	2020
ISSN:	0162-0134 1873-3344
Megjegyzések:	Based on our previous works involving two 1,4,7-triazacyclononane (tacn)-based ligands Hno2py1pa (1-Picolinic acid-4,7-bis(pyridin-2-ylmethyl)-1,4,7-triazacyclononane) and Hno1pa (1-Picolinic acid-1,4,7-triazacyclononane), we report here the synthesis of analogues bearing picolinate-based rz-conjugated ILCT (IntraLigand Charge Transfer) transition antenna (HL1, HL2), using regiospecific N-functionalization of the tacn skeleton and their related transition metal complexes (e.g. Cu2+, Zn2+ and Mn2+). Coordination properties as well as their photophysical and electrochemical properties were investigated in order to quantify the impact of such antenna on the luminescent or relaxometric properties of the complexes. The spectroscopic properties of the targeted ligands and metal complexes have been studied using UV-Vis absorption and fluorescence spectrocopies. While the zinc complex formed with HL1 possesses a moderate quantum yield of 5%, complexation of Cu2+ led to an extinction of the luminescence putatively attributed to a photo-induced electron transfer, as supported by spectroscopic and electrochemical evidences. The [Mn(L2)](+) complex is characterized by a fluorescence quantum yield close to 8% in CH2Cl2. The potential interest of such systems as bimodal probes has been assessed from radiolabeling experiments conducted on HL1 and( 64)Cu(2+) as well as confocal microscopy analyses and from relaxometric studies carried out on the cationic [Mn(L2)](+) complex. These results showed that HL1 can be used for radiolabeling, with a radiochemical conversion of 40% in 15 min at 100 degrees C. Finally, the relaxivity values obtained for [Mn(L2)](+), r(1p) = 4.80 mM(-1).s(-1) and r(2p) = 8.72 mM(-1).s(-1), make the Mn(II) complex an ideal candidate as a probe for Magnetic Resonance Imaging.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk
Megjelenés:	Journal of Inorganic Biochemistry. - 205 (2020), p. 1-9. -
További szerzők:	Galland, Margaux Roux, Amandine Váradi Balázs (1990-) (vegyész) Gogolák Réka Anna (kémia tanár) Le Saëc, Patricia Faivre-Chauvet, Alain Beyler, Maryline Bucher, Christophe Tircsó Gyula (1977-) (vegyész, kémia tanár) Patinec, Véronique Maury, Olivier Tripier, Raphaël
Pályázati támogatás:	NKFIH-K-120224 Egyéb GINOP-2.3.2-15-2016-00008 GINOP
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001-es BibID:	BIBFORM103038
035-os BibID:	(wos)000481917100005 (scopus)85071026081
Első szerző:	Tircsó Gyula (vegyész, kémia tanár)
Cím:	Dialing in on pharmacological features for a therapeutic antioxidant small molecule / Green Kayla N., Pota Kristof, Tircsó Gyula, Gogolák Réka Anna, Kinsinger Olivia, Davda Collin, Blain Kimberly, Brewer Samantha M. Gonzalez Paulina, Johnston Hannah M., Akkaraju Giridhar
Dátum:	2019
ISSN:	1477-9226
Megjegyzések:	The pyridinophane molecule L2 (3,6,9,15-tetraazabicyclo[9.3.1]penta-deca-1(15),11,13-trien-13- ol) has shown promise as a therapuetic for neurodegenerative diseases involving oxidative stress and metal ion misregulation. Protonation and metal binding stability constants with Mg2+, Ca2+, Cu2+, and Zn2+ ions were determined to further explore the therapeutic and pharmacological potential of this water soluble small molecule. These studies show that incorporation of an ?OH group in position 4 of the pyridine ring decreases the pI values compared to cyclen and L1 (3,6,9,15-tetraazabicyclo[9.3.1]penta-deca-1(15),11,13-triene). Furthermore, this approach tunes the basicity of the tetra-aza macrocyclic ligand through the enhanced resonance stabilization of the ?OH in position 4 and rigidity of the pyridine ring such that L2 has increased basicity compared to previously reported tetra-aza macrocycles. A metal binding preference for Cu2+, a redox cycling agent known to produce oxidative stress, indicates that this would be the in vivo metal target of L2. However, the binding constant of L2 with Cu2+ is moderated compared to cyclen due to the rigidity of the ligand and shows how ligand design can be used to tune metal selectivity. An IC50=298.0 ?M in HT-22 neuronal cells was observed. Low metabolic liability was determined in both Phase I and II in vitro models. Throughout these studies other metal binding systems were used for comparison and as appropriate controls. The reactivity reported to date and pharmacological features described herein warrant further studies in vivo and the pursuit of L2 congeners using the knowledge that pyridine substitution in a pyridinophane can be used to tune the structure of the ligand and retain the positive therapeutic outcomes.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk Ligand Pyridinophane tetra-aza macrocycle binding transition metal-ion
Megjelenés:	Dalton Transactions. - 48 : 33 (2019), p. 12430-12439. -
További szerzők:	Green, Kayla N. Póta Kristóf Gogolák Réka Anna (kémia tanár) Olivia Kinsinger Collin Davda Kimberly Blaina Samantha M. Brewer Paulina Gonzalez Hannah M. Johnston Giridhar Akkarajuc
Pályázati támogatás:	(NKFIH K-120224) MTA ÚNKP-18?4 N Egyéb GINOP-2.3.2-15-2016-00008 GINOP GINOP-2.3.3-15-2016-00004 GINOP
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