[en] Central to the production of new antibody-conjugated radioisotopes for diagnostic or therapeutic use is the development of fundamental main-group and inorganic chemistry. In this respect, ¹⁰⁹Pd is an attractive isotope for radioimmunotherapy. It has a suitable half-life (13.1 hr) and suitable physical properties (β=1.02 MeV, 100%). It decays to a 40 sec half-life ¹⁰⁹Ag which emits an 88 keV γ, making it suitable for imaging. The authors' approach to this endeavor involves the application of functionalized phosphorus hydrazides which form kinetically robust complexes with transition metals/metallic radioisotopes. The -COOH functionality in the bifunctional chelate after activation can be used to conjugate onto peptides/proteins to generate a new genre of metal-conjugated biomolecules for applications in nuclear medicine. The synthesis, spectroscopic and X-ray crystallographic analysis of bifunctional chelates are discussed

[en] Short communication

[en] Short communication

[en] A new bis-hydrazide-phosphine (BHP) ligand was synthesized, characterized and complexed with ^99mTc. ^99mTc phenyl-BHP (PBHP) was shown to form a neutral-lipophilic chelate with ^99mTc, in high yields, that is stable over a wide pH range. Results with ^99mTc-PBHP indicate that the BHP chelating moiety is attractive for use in designing new ^99mTc-imaging agents. (author)

[en] We report herein an innovative approach to prostate tumor therapy using tumor specific radioactive gold nanoparticles (¹⁹⁸Au) functionalized with Mangiferin (MGF). Production and full characterization of MGF-¹⁹⁸AuNPs are described. In vivo therapeutic efficacy of MGF-¹⁹⁸AuNPs, through intratumoral delivery, in SCID mice bearing prostate tumor xenografts are described. Singular doses of the nano-radiopharmaceutical (MGF-¹⁹⁸AuNPs) resulted in over 85% reduction of tumor volume as compared to untreated control groups. The excellent anti-tumor efficacy of MGF-¹⁹⁸AuNPs are attributed to the retention of over 90% of the injected dose within tumors for long periods of time. The retention of MGF-¹⁹⁸AuNPs is also rationalized in terms of the higher tumor metabolism of glucose which is present in the xanthanoid functionality of MGF. Limited/no lymphatic drainage of MGF-¹⁹⁸AuNPs to various non-target organs is an attractive feature presenting realistic scope for the clinical translation of MGF-¹⁹⁸AuNPs in for treating prostate cancers in human patients. The comparative analysis of MGF-¹⁹⁸AuNPs with other radioactive gold nanoparticles, functionalized either with epigallocatechin gallate or the Gum Arabic, has revealed significantly superior tumoricidal characteristics of MGF-¹⁹⁸AuNPs, thus corroborating the importance of the tumor-avid glucose motif of MGF. Oncological implications of MGF-¹⁹⁸AuNPs as a new therapeutic agent for treating prostate and various solid tumors are presented. (author)

[en] Azaphosphanes functionalized with different organic substituents have been shown to selectively scavenge ^99mTcO₄^- in the presence of different concentrations of anions (NO₃^-, Cl^-, OH^-) and cations (Pd²⁺, Pt²⁺, Fe³⁺). The fundamental coordination chemistry of the azaphosphane-based ligand systems with Re included detailed NMR spectroscopic and X-ray structural investigations which has provided important insights that may aid in the application of new azaphosphane ligands for scavenging specific transition metals. The aforementioned studies, clearly show the potential for the application of this new class of main group monomers and polymers in the treatment of liquid wastes containing ⁹⁹TcO₄^- for use in waste management procedures. (orig.)

[en] Ph₃PNSiMe₃ reacts with ^99mTcO₄^- to form an ion pair that is soluble in organic solvents. Heating of the ion pair produces a new ^99mTc species that is neutral and lipophillic and stable in dry toluene for ≥ 2h. Dissolving this new complex in 1:1, EtOH:H₂O results in conversion of the product back to the ion pair which will limit its in vitro and in vivo stability. The chromatographic properties of the ion pair and the ^99mTc species produced when heated in toluene are similar to the analogous Re complexes with Ph₃PNSiMe, which should have the following respective structures: [Ph₃PNH₂⁺][^99mTcO₄^-] and Ph₃PN^99m TcO₃. These results indicate the potential of phosphinimine ligands in formulation of new ^99mTc radiopharmaceuticals, particularly if phosphinimine ligand derivatives are developed that provide substantially improved stability of the respective complexes in aqueous solutions. (author)

[en] Reactions of the organometallic phosphinimine Ph₃P=N-SiMe₃ (1), with aqueous ReO₄^- and ¹⁸⁸ReO₄^- yield the ion pairs Ph₃P=NH₂⁺NO₄^-(M=Re (2); ¹⁸⁸Re (4)). The ion pairs undergo dehydration upon heating to produce the neutral Re (VII) species: Ph₃P=N-MO₃(M=Re (3); ¹⁸⁸Re (5)). The solid state structure of Ph₃P=NH₂⁺ReO₄^- (2) shows the presence of hydrogen bonding between the iminato hydrogen and the rhenium oxo center. The relevance of such reactions for the design of new radiopharmaceuticals is discussed. (orig.)