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Comparative in vivo stability of copper-64-labeled cross-bridged and conventional tetraazamacrocyclic complexes.
Results indicate that the structurally reinforcing cross-bridge enhances in vivo stability by reducing metal loss to protein in both the cyclam and cyclen cross-bridged (64)Cu complexes and that ( 64)Cu-CB-TE2A is superior to (64)-CB-DO2A in that regard. Expand
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses
A robust diastereoselective synthesis provided sufficient quantities of 4b to enable preclinical efficacy in a non-human-primate EBOV challenge model and structure activity relationships established that the 1′-CN group and C-linked nucleobase were critical for optimal anti-EBOV potency and selectivity against host polymerases. Expand
Synthesis and Characterization of Cross-Bridged Cyclams and Pendant-Armed Derivatives and Structural Studies of Their Copper(II) Complexes
A series of 1,4,8,11-tetraazabicyclo[6.6.2]hexadecane ligands, including the parent compound, N,N‘-dialkyl variants, and the first N,N‘-di-pendant-arm derivatives have been synthesized by a short,Expand
Lynamicins A-E, chlorinated bisindole pyrrole antibiotics from a novel marine actinomycete.
A series of chlorinated bisindole pyrroles, lynamicins A-E (1-5), was discovered from a novel marine actinomycete, NPS12745, which was isolated from a marine sediment collected off the coast of San Diego, California, which demonstrated that these substances possess broad-spectrum activity against both Gram-positive and Gram-negative organisms. Expand
Synthesis, characterization and in vivo studies of Cu(II)-64-labeled cross-bridged tetraazamacrocycle-amide complexes as models of peptide conjugate imaging agents.
Clearance of 64Cu-cross-bridged monoamides from nontarget organs suggests good in vivo stability, thus supporting the use of CB-TE2A as a bifunctional chelator without modifications to the macrocycle backbone. Expand
A functional model for O-O bond formation by the O2-evolving complex in photosystem II.
Oxygen-18 isotope labeling showed that water is the source of the oxygen atoms in the molecular oxygen evolved, and so this system is a functional model for photosynthetic water oxidation. Expand
Synthesis of (-)-morphine.
The preparation of the diastereomerically pure beta-tetralone ketal 4 is reported and the key step in this synthesis was the bis-intramolecular cyclization of keto aldehyde 2 to give the tetracyclic intermediate 20. Expand
Napyradiomycin derivatives, produced by a marine-derived actinomycete, illustrate cytotoxicity by induction of apoptosis.
Using fluorescence-activated cell sorting (FACS) analysis, napyradiomycins 1-4 were observed to induce apoptosis in the colon adenocarcinoma cell line HCT-116, indicating the possibility of a specific biochemical target for this class of cytotoxins. Expand
Syntheses of tris(pyrazolyl)methane ligands and {[tris(pyrazolyl)methane]Mn(CO)3}SO3CF3 complexes: comparison of ligand donor properties
Abstract The known ligands HC(pz)3, HC(3,5-Me2pz)3, HC(3-Phpz)3, and HC(3-tBupz)3 and the new ligand HC(3-iPrpz)3 (pz=pyrazolyl ring) are prepared in CHCl3–H2O using the appropriate pyrazole, anExpand