title: Ester-modified 99mTcO[SN(R)S/S] mixed ligand complexes: synthesis and preliminary evaluation.
abstract: Two novel 99mTc-(SNS/S) complexes: a mono-ester compound carrying an ethyl ester group on the tridentate ligand, 99mTcO[C(2)H(5)OOCCH(2)N(CH(2)CH(2)S)(2)][SC(6)H(4)CH(3)], 3, and a diester compound, carrying a second ethyl ester group on the monodentate ligand, 99mTcO[C(2)H(5)OOCCH(2)N(CH(2)CH(2)S)(2)][SC(6)H(4)COOC(2)H(5)], 4, were synthesized. The corresponding oxorhenium(V) complexes, 1 and 2 were also synthesized. Enzymatic hydrolysis demonstrated that 3 remains intact after 10 min incubation while 4 is totally converted to an unidentified hydrophilic complex. Tissue distribution data in mice revealed that both complexes, 3 and 4, exhibit significant initial brain uptake (1.42 and 1.01% of injected dose at 5 minutes post injection respectively) and fast blood clearance.
authors.affiliation: Institute of Radioisotopes-Radiodiagnostic Products, National Center for Scientific Research Demokritos, 15310 Ag. Paraskevi, Athens, Greece.
authors.forename: C
authors.initials: C
authors.lastname: Tsoukalas
authors.forename: I
authors.initials: I
authors.lastname: Pirmettis
authors.forename: G
authors.initials: G
authors.lastname: Patsis
authors.forename: A
authors.initials: A
authors.lastname: Papadopoulos
authors.forename: C P
authors.initials: CP
authors.lastname: Raptopoulou
authors.forename: A
authors.initials: A
authors.lastname: Terzis
authors.forename: M
authors.initials: M
authors.lastname: Papadopoulos
authors.forename: E
authors.initials: E
authors.lastname: Chiotellis
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism; D004952:Esters; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D017556:Technetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D014018:Tissue Distribution
chemical_list: D004952:Esters; D017556:Technetium Compounds