Theranostic inorganic-organic hybrid nanoparticles with a cocktail of chemotherapeutic and cytostatic drugs.

Theranostic inorganic-organic hybrid nanoparticles (IOH-NPs) with a cocktail of chemotherapeutic and cytostatic drugs and a composition Gd[(PMX)(EMP)], [Gd(OH)][(PMX)(AlPCS)], or [Gd(OH)][(PMX)(TPPS)] (PMX: pemetrexed, EMP: estramustine phosphate, AlPCS: aluminum(III) chlorido phthalocyanine tetrasulfonate, TPPS: tetraphenylporphine sulfonate) are presented for the first time. These IOH-NPs are prepared in water (40-60 nm in size) and have a non-complex composition with outstanding drug loading (71-82% of total nanoparticle mass) of at least two chemotherapeutic or a mixture of cytostatic and photosensitizing agents. All IOH-NPs show red to deep-red emission (650-800 nm) to enable optical imaging.

Cyclic Peptoid-Peptide Hybrids as Versatile Molecular Transporters.

Addressing intracellular targets is a challenging task that requires potent molecular transporters capable to deliver various cargos. Herein, we report the synthesis of hydrophobic macrocycles composed of both amino acids and peptoid monomers. The cyclic tetramers and hexamers were assembled in a modular approach using solid as well as solution phase techniques.

Total synthesis of decarboxyaltenusin.

The total synthesis of decarboxyaltenusin (5'-methoxy-6-methyl-[1,1'-biphenyl]-3,3',4-triol), a toxin produced by various mold fungi, has been achieved in seven steps in a yield of 31% starting from 4-methylcatechol and 1-bromo-3,5-dimethoxybenzene, where the longest linear sequence consists of five steps. The key reaction was a palladium-catalyzed Suzuki coupling of an aromatic boronate with a brominated resorcin derivative.

Synthesis, Characterization, and Biological Properties of Steroidal Ruthenium(II) and Iridium(III) Complexes Based on the Androst-16-en-3-ol Framework.

A range of novel cyclometalated ruthenium(II) and iridium(III) complexes with a steroidal backbone based on androsterone were synthesized and characterized by NMR spectroscopy and X-ray crystallography. Their cytotoxic properties in RT112 and RT112 cP (cisplatin-resistant) cell lines as well as in MCF7 and somatic fibroblasts were compared with those of the corresponding nonsteroidal complexes and the noncyclometalated pyridyl complexes as well as with cisplatin as reference. All steroidal complexes were more active in RT112 cP cells than cisplatin, whereby the cyclometalated pyridinylphenyl complexes based on showed high cytotoxicity while maintaining low resistant factors of 0.

Fluorescent Sulfonate-Based Inorganic-Organic Hybrid Nanoparticles for Staining and Imaging.

Sulfonate-based inorganic-organic hybrid nanoparticles (IOH-NPs) with the general saline composition [Gd(OH)][ R(SO) ] showing optical absorption and emission in the blue to red spectral regime are presented for the first time. All IOH-NPs are prepared via straightforward aqueous synthesis and instantaneously result in colloidally highly stable suspensions with mean particle diameters of 40-50 nm and high zeta potentials (-20 to -40 mV at pH 7.0).