Black graphitic carbon nitride nanosheets with mid-gap states realizing highly efficient near-infrared photo-thermal conversion for photoacoustic imaging.

Developing metal-free photo-thermal transduction nanoagents (PTNAs) with high conversion efficiency addresses the balance between superior photothermal performance and good biocompatibility in the field of bio-applications of PTNAs. Herein, we highlight the bandgap-engineered black graphitic carbon nitride nanosheets (denoted as B-g-CN) as a novel metal-free PTNA with high conversion efficiency (62% at 808 nm) for photoacoustic imaging. The B-g-CN absorbed infrared light with a narrowed bandgap and electronic states within the band (known as mid-gap states) due to the synergistic effect of sulfur incorporation, nitrogen vacancies and the porous structure.

Synthesis, antitumor activity evaluation and mechanistic study of novel hederacolchiside A derivatives bearing an aryl triazole moiety.

In an attempt to arrive at a more potent antitumor agent than the parent natural saponin hederacolchiside A, 23 hederacolchiside A derivatives (4a-4w) were synthesized via Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition and screened in vitro for cytotoxicity against six human cancer cell lines. The structure-activity relationship of these compounds was elucidated, and the biological screening results showed that most of the compounds exhibited moderate to high levels of antitumor activities against the tested cell lines and some of them displayed more potent inhibitory activities compared with hederacolchiside A. Compound 4f showed a 2- to 7-fold more potent activity than hederacolchiside A.

Synthesis, biological evaluation and molecular modeling of 2-amino-2-phenylethanol derivatives as novel β-adrenoceptor agonists.

A novel series of 2-amino-2-phenylethanol derivatives were developed as β-adrenoceptor agonists. Among them, 2-amino-3-fluoro-5-(2-hydroxy-1-(isopropylamino)ethyl)benzonitrile (compound 2f) exhibited the highest activity (EC = 0.25 nM) in stimulating β-adrenoceptor-mediated cellular cAMP production with a 763.

Synthesis and biological evaluation of β-adrenoceptor agonists bearing the 2-amino-2-phenylethanol scaffold.

A new series of β-adrenoceptor agonists bearing the 2-amino-2-phenylethanol scaffold was synthesized. Evaluation of the compounds using cell assays and an in vitro guinea pig trachea relaxation assay showed that 8-hydroxy-5-(2-hydroxy-1-((4-hydroxyphenethyl)amino)ethyl)quinolin-2(1H)-one (compound 5j) has the best pharmacological profile among all the evaluated compounds. The (S)-isomer of 5j was subsequently found to be the active enantiomer with a promising EC value of 1.

Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site.

Dual-tail approach was employed to design novel Carbonic Anhydrase (CA) IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site, which also contains a zinc ion as part of the catalytic center. The classic sulfanilamide moiety was used as the zinc binding group. An amino glucosamine fragment was chosen as the hydrophilic part and a cinnamamide fragment as the hydrophobic part in order to draw favorable interactions with the corresponding halves of the active site.