Joseph A. Ioppolo

The first indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing carborane

Indoleamine-2,3-dioxygenase-1 (IDO1) is a critical immunoregulatory enzyme responsible for the metabolism of tryptophan during inflammation and disease. Based upon a pyranonaphthoquinone framework, the first examples of indoleamine-2,3-dioxygenase-1 (IDO1) inhibitors containing a carborane cage are reported. The novel closo-1,2-carboranyl-N-pyranonaphthoquinone derivatives display low μM binding affinity for the human recombinant enzyme, with IC50 values ranging from 0.78 to 1.77 μM.

Mono- and Di-nuclear Gold(i) Complexes Containing 1,12-Dicarba-closo-dodecaborane(12)

The first examples of gold(i) complexes containing monodentate diphenylphosphine-1,12-carborane and bidentate 1,12-bis(diphenylphosphine)-1,12-carborane ligands are reported.

Remarkable cage deboronation and rearrangement of a closo-1,12-dicarbadodecaborane to form a neutral nido-7,9-dicarbaundecaborane

Deboronation and cage rearrangement of the closo-1,12-carborane salt [1,12-(PPh2Me)2-1,12-C2B10H10]I2 occurs in refluxing methanol to give the zwitterionic nido-7,9-carborane 7,9-(PPh2Me)2-7,9-C2B9H9. Notably, deboronation and cage substitution of the isomeric closo-1,7-carborane salt [1,7-(PPh2Me)2-1,7-C2B10H10]I2 takes place in methanol to afford the salt [10-OMe-7,9-(PPh2Me)2-7,9-C2B9H9]I.

Boron and Gadolinium Neutron Capture Therapy

This chapter reviews the current state of the art in an experimental cancer treatment known as neutron capture therapy (NCT) with a strong emphasis on the chemistry and biology of selected NCT agents containing boron and/or gadolinium.

[1,2-Bis(diphenyl­phosphino)-1,2-dicarba-closo-dodeca­borane-κ2P,P′][7,8-bis­(di­phenyl­phosphino)-7,8-dicarba-nido-undeca­borato-κ2P,P′]gold(I)–dichloro­methane–water (2/1/1)

The title compound, [Au(C26H30B10P2)(C26H30B9P2)]·0.5CH2Cl2·0.5H2O, contains two independent complex molecules in the asymmetric unit. The gold(I) centres display a distorted tetrahedral geometry. The complex is stablized through weak intramolecular π–π stacking (Cg⋯Cg = 4.17 Å) and edge-to-face interactions (H⋯Cg = 3.21 Å). Adjacent molecules interact through C—H⋯π (H⋯Cg = 2.88 Å) and B—H⋯π (H⋯Cg = 3.15 Å) contacts, forming a three-dimensional network, with solvent molecules occupying the cavities. One of the phenyl groups was disordered over two sites with occupancy factors of 0.65 and 0.35.