5,5-Dimethyl-2-methyl­seleno-1,3,2-dioxaphospho­rinan-2-one

The title compound, C6H13O3PSe, was obtained in the reaction of 5,5-dimethyl-2-oxo-2-seleno-1,3,2-dioxaphospho­r­inane potassium salt with methyl iodide. The seleno­methyl group is in the axial position in relation to the six-membered dioxaphospho­rinane ring

O-Pivaloyl diphenyl­seleno­phosphinate

The title compound, C17H19O2PSe, was obtained in the reaction of the diphenyl­monoseleno­phosphinic acid ammonium salt with pivaloyl chloride. The P—Se bond length of 2.0769 (11) Å is normal, while the P—O bond length of 1.650 (3) Å is longer than in related O-alkyl and O-aryl derivatives. One phenyl ring is periplanar to the Se—P—C plane, while the dihedral angle between the two phenyl rings is ca 73°. The carbonyl group is in a synperiplanar position [torsion angle = 8.9 (6)°] to one of the methyl groups of the pivaloyl group. This is the first O-acyl derivative of diphenyl­monoseleno­phosphinic acid characterized by X-ray structural analysis

O-4-Chloro­benzoyl diphenyl­seleno­phosphinate

The title compound, C19H14ClO2PSe, was obtained in the reaction of the diphenyl­monoseleno­phosphinic acid ammonium salt with 4-chloro­benzoyl chloride. The dihedral angle between the P-bonded aromatic rings is 72.64 (14)°. Packing of the mol­ecules in the crystal is reinforced by π–π stacking inter­actions between two inversion-related 4-chloro­benzene rings [centroid-centroid separation = 4.189 (2) Å] and a C—H⋯O interaction also occurs

Novel 1,2,4-Oxadiazole Derivatives in Drug Discovery

Five-membered 1,2,4-oxadiazole heterocyclic ring has received considerable attention because of its unique bioisosteric properties and an unusually wide spectrum of biological activities. Thus, it is a perfect framework for the novel drug development. After a century since the 1,2,4-oxadiazole have been discovered, the uncommon potential attracted medicinal chemists’ attention, leading to the discovery of a few presently accessible drugs containing 1,2,4-oxadiazole unit. It is worth noting that the interest in a 1,2,4-oxadiazoles’ biological application has been doubled in the last fifteen years. Herein, after a concise historical introduction, we present a comprehensive overview of the recent achievements in the synthesis of 1,2,4-oxadiazole-based compounds and the major advances in their biological applications in the period of the last five years as well as brief remarks on prospects for further development

Recent progress in the development of steroid sulphatase inhibitors – examples of the novel and most promising compounds from the last decade

The purpose of this review article is to provide an overview of recent achievements in the synthesis of novel steroid sulphatase (STS) inhibitors. STS is a crucial enzyme in the biosynthesis of active hormones (including oestrogens and androgens) and, therefore, represents an extremely attractive molecular target for the development of hormone-dependent cancer therapies. The inhibition of STS may effectively reduce the availability of active hormones for cancer cells, causing a positive therapeutic effect. Herein, we report examples of novel STS inhibitors based on steroidal and nonsteroidal cores that contain various functional groups (e.g. sulphamate and phosphorus moieties) and halogen atoms, which may potentially be used in therapies for hormone-dependent cancers. The presented work also includes examples of multitargeting agents with STS inhibitory activities. Furthermore, the fundamental discoveries in the development of the most promising drug candidates exhibiting STS inhibitory activities are highlighted