Aim: To explore the therapeutic effect of nanoparticle-based dual-targeting delivery of antitumor agents for glioblastoma treatment. Materials & methods: A hepatitis B core protein-virus-like parti...

To accomplish effective cancer imaging and integrated therapy, the multifunctional nanotheranostic Fe₃O₄-MTX@HBc core-shell nanoparticles (NPs) were designed. A straightforward method was demonstrated for efficient encapsulation of magnetic NPs into the engineered virus-like particles (VLPs) through the affinity of histidine tags for the methotrexate (MTX)-Ni²⁺ chelate. HBc₁₄₄-His VLPs shell could protect Fe₃O₄-MTX NPs from the recognition by the reticuloendothelial system as well as could increase their cellular uptake efficiency. Through our well-designed tactic, the photothermal efficiency of Fe₃O₄ NPs were obviously improved in vitro and in vivo upon near-infrared (NIR) laser irradiation. Moreover, Magnetic resonance imaging (MRI) results showed that the Fe₃O₄-MTX@HBc core-shell NPs were reliable T₂-type MRI contrast agents for tumor imaging. Hence the Fe₃O₄-MTX@HBc core-shell NPs may act as a promising theranostic platform for multimodal cancer treatment.

Kinases are among the most important families of biomolecules and play an essential role in the regulation of cell proliferation, apoptosis, metabolism, and other critical physiological processes. The dysregulation and gene mutation of kinases are linked to the occurrence and development of various human diseases, especially cancer. As a result, a growing number of small-molecule drugs based on kinase targets are being successfully developed and approved for the treatment of many diseases. The indole/azaindole/oxindole moieties are important key pharmacophores of many bioactive compounds and are generally used as excellent scaffolds for drug discovery in medicinal chemistry. To date, 30 ATP-competitive kinase inhibitors bearing the indole/azaindole/oxindole scaffold have been approved for the treatment of diseases. Herein, we summarize their research and development (R&D) process and describe their binding models to the ATP-binding sites of the target kinases. Moreover, we discuss the significant role of the indole/azaindole/oxindole skeletons in the interaction of their parent drug and target kinases, providing new medicinal chemistry inspiration and ideas for the subsequent development and optimization of kinase inhibitors.

Detailed chemical investigation of the South China sponge Dysidea arenaria resulted in the isolation of a new sesquiterpenoid hydroquinone, 19-hydroxypolyfibrospongol B (1), along with five known compounds: polyfibrospongol B (2), isosemnonorthoquinone (3), ilimaquinone (4), smenospongine (5) and smenotronic acid (6). The structures were determined by extensive spectroscopic analysis. The in vitro anti- HIV activity on HIV-1 RT was evaluated. Compounds 3 -6 displayed moderate inhibitory activity, with IC₅₀ values of 239.7, 16.4, 176.1, and 130.4 μM, respectively, while 1 and 2 were found to be inactive against the same biological target.