A novel series of PI3Kβ (Phosphatidylinositol-3-kinases beta subunit) inhibitors with the structure of benzothiazole scaffold have been designed and synthesized. All the compounds have been evaluated for inhibitory activities against PI3Kα, β, γ, δ and mTOR (Mammalian target of rapamycin). Two superior compounds have been further evaluated for the IC50 values against PI3Ks/mTOR. The most promis...

New pH-activatable ratiometric fluorescent probes have been developed that have a coumarin structure attached to benzothiazole or indole units with one or two conjugated bonds. They have optical responses in acidic conditions. Probes with benzothiazole (1) and indole (2, 3) units have opposite responses to changes in pH, in terms of shifts in absorption and emission. Quantum chemical calculatio...

This paper describes a simple route to enantiomerically enriched [2.2]paracyclophane-4-thiol via the stereospecific introduction of a chiral sulfoxide to the [2.2]paracyclophane skeleton. The first synthesis of an enantiomerically enriched planar chiral benzothiazole is also reported.

Aryl-substituted benzothiazoles and benzoxazoles are an important class of heterocyclic compound and have shown a wide range of biological activities, such as antitumor, antiviral, and antimicrobial activities. In addition, these compounds have become essential building blocks for the synthesis of conjugated functional materials, such as industrial dyes and plant growth regulators. The conventi...

Neurleptic drugs, e.g., aripiprazole, targeting the dopamine D2S and D3 receptors (D2SR and D3R) in the central nervous system are widely used in the treatment of several psychotic and neurodegenerative diseases. Therefore, a new series of benzothiazole-based ligands (3-20) was synthesized by applying the bioisosteric approach derived from the selective D3Rs ligand BP-897 (1) and its structural...

Recently we reported the preparation and properties of some 2-(2or · 3-furyl)benzothiazoles1• Like many other thiazoles2 , due to their weak basic character they can give quaternary salts. Comparing 2-(2-methyl-3-furyl)benzothiazoles with the 2-(5-methyl-2-furyl) analogue it was observed that the nucleophilicity (and basicity) of benzothiazole nitrogen is influenced by the position of the methy...

Complexation of a boron atom with two of benzothiazole-enolate-based bidentate ligands successfully gave rise to the corresponding BF2-/BPh2-chelated complexes (), which could be considered as novel AIE-active organoboron luminophores. These new luminophores exhibited aggregation-induced emission, and a large Stokes shift in solution. In the solid-state, compounds exhibited intense emission wit...

Dicarba-closo-dodecaboranes, commonly known as carboranes, possess unique physico-chemical properties and can be used as hydrophobic moieties during the design of new drugs or radiotracers. In this work, we report the synthesis of two analogues of 2-(4-aminophenyl)benzothiazole (a compound that was found to elicit pronounced inhibitory effects against certain breast cancer cell lines in vitro) ...

Ir(III) complexes that contain benzothiazole-based tridentate ligands were synthesized and their crystal structures and luminescent properties were examined. A neutral complex had a high quantum yield (89%) and performed well as an emissive material for organic light-emitting diodes.

The coordination chemistry of 2,5-dicarbothioamidopyrrole ligands, namely N2,N5-dibutyl-3,4-diphenyl-1H-pyrrole-2,5-bis(carbothioamide) and N2,N5,3,4-tetraphenyl-1H-pyrrole-2,5-bis(carbothioamide), has been investigated with Cu(II) metal centres by means of X-ray crystallography. This resulted in the formation of the expected planar S,N,S' coordinated complex for the former ligand and unexpecte...