Molecular docking for affinity calculations was performed using the AutoDock software. This research aimed to design, synthesize and preclinically evaluate a new FAP inhibitor radiopharmaceutical based on the 99mTc-((R)-1-((6-hydrazinylnicotinoyl)-D-alanyl) pyrrolidin-2-yl) boronic acid (99mTc-iFAP) structure for SPECT imaging. 68Ga-labeled FAP inhibitors based on the cyanopyrrolidine structure (FAPI) are currently used for the detection of the tumor microenvironment by PET imaging. This contribution intends to highlight the potential of pyrazolyl-containing chelators for the labeling of biologically active molecules with 99mTc(I), being presented a variety of examples which include peptides, peptide nucleic acids, inhibitors/substrates of enzymes and DNA-binders.įibroblast activation protein (FAP) is expressed in the microenvironment of most human epithelial tumors. The revised work focuses mainly on tricarbonyl M(I) complexes but M(V) oxocomplexes are also covered. Such research efforts are reviewed herein, where we present an overview of the chemistry, radiochemistry and biological properties of Re and 99mTc complexes anchored by those pyrazolyl-containing chelators with relevance in radiopharmaceutical research. Owing to our interest on the design of innovative target-specific radioactive probes, we have been recently involved in the study of the chemistry of 3+ and fac-+ (M = Re, Tc) with chelators combining a pyrazolyl unit with aliphatic amines and/or carboxylic acids or thioethers. More recently, the remarkable features of the organometallic precursor fac- + (M = Re, Tc), introduced by Alberto et al., brought renewed interest in the design of innovative lowoxidation 99mTc-based radiopharmaceuticals. Among all oxidation states available for technetium (-I to VII), the V oxidation state has been the most extensively studied in radiopharmaceutical chemistry, and the majority of the 99mTc-radiopharmaceuticals in clinical use contain the core 3+. The design of novel target-specific imaging agents based on 99mTc requires a considerable development of its coordination chemistry.

Motocross nitro unblocked 666