Chemo- and Regioselective Alkylation of Pyridine -Oxides with Titanacyclopropanes.

While titanacyclopropanes are used to react mainly with ester, amide, and cyano to undergo cyclopropanation, herein they react preferentially with pyridine -oxide to accomplish C2-H alkylation beyond these functionalities with double regioselectivity. After being pyridylated at the less hindered C-Ti bond, the remaining C-Ti bond of titanacyclopropanes can be further functionalized by various electrophiles, allowing facile introduction of complex alkyls onto the C2 of pyridines. Its synthetic potential has been demonstrated by late-stage diversification of drugs.

Conditional knockout of ITGB4 in bronchial epithelial cells directs bronchopulmonary dysplasia.

Neonatal respiratory system disease is closely associated with embryonic lung development. Our group found that integrin β4 (ITGB4) is downregulated in the airway epithelium of asthma patients. Asthma is the most common chronic respiratory illness in childhood.

Fe-Catalyzed Difunctionalization of Aryl Titanates Enabled by Fe/Ti Synergism.

Fe-catalyzed difunctionalization of aryl titanates via double C-H activation has been developed, where aryl titanates were arylated via C-H activation, followed by electrophilic trapping of the C-Ti bond. The C-H arylation should be promoted by a 1,2-Fe/Ti synergistic heterobimetallic arylene intermediate and represents an C-H ferration directed by a readily transformable C-Ti group. Common benzamides, esters, and nitriles function as arylating reagents, which involves another C-H activation directed by these functionalities.

Synergism of Fe/Ti Enabled Regioselective Arene Difunctionalization.

Regioselective difunctionalization of arenes remains a long-standing challenge in organic chemistry. We report a novel and general Fe/Ti synergistic methodology for regioselective synthesis of various polysubstituted arenes through either E/E' or Nu/E difunctionalizations of arenes. Preliminary results showed that an unprecedented 1,2-Fe/Ti heterobimetallic arylene intermediate bearing two distinct C-M bonds is essential to the regioselective difunctionalization.

Airway epithelial integrin β4-deficiency exacerbates lipopolysaccharide-induced acute lung injury.

Airway epithelial cells, the first barrier of the respiratory tract, play an indispensable role in innate immunity. Integrin β4 (ITGB4) is a structural adhesion molecule that is involved in the pathological progression of acute inflammatory diseases and is downregulated in asthmatic patients. Research has shown that endothelial ITGB4 has proinflammatory properties in acute lung injury (ALI).

Diversity and Bioactivity of Endophytes From in China.

Plant seeds are not merely reproductive organs, they are also carriers of microorganism, particularly, inherent and non-invasive characteristic endophytes in host plant. Therefore, in this study, the endophytic diversity of seeds was studied and compared with endophytes isolated from healthy leaves, stems, roots, and seeds of . using 20 different media.

Iron-catalyzed stereospecific arylation of enol tosylates using Grignard reagents.

The stereospecific Fe-catalyzed arylation of enol tosylates was reported. Various tri- or tetrasubstituted Z or E-enol tosylates of β-keto esters were arylated using common and Knochel-type Grignard reagents with complete stereofidelity. The precursors for Z/E-zimelidine, tamoxifen and other bioactive compounds were facilely prepared without precious and toxic transition metals.

A new mixed inhibitor of adenosine deaminase produced by endophytic Cochliobolus sp. from medicinal plant seeds.

Medicinal plants have been studied for potential endophytic interactions and numerous studies have provided evidence that seeds harbor diverse microbial communities, not only on their surfaces but also within the embryo. Adenosine deaminase (ADA) is known as a potential therapeutic target for the treatment of lymphoproliferative disorders and cancer. Therefore, in this study, 20 types of medicinal plant seeds were used to screen endophytic fungi with tissue homogenate and streak.

Reynoutria Japonica from Traditional Chinese Medicine: A Source of Competitive Adenosine Deaminase Inhibitors for Anticancer.

Background: Adenosine deaminase (ADA) is an important enzyme in purine metabolism and is known as a potential therapeutic target for the treatment of lymphoproliferative disorders and cancer. Traditional Chinese Herbal Medicine (TCHM) is widely used alone or in combination with chemotherapy to treat cancer, due to its ability to deliver a broad variety of bioactive secondary metabolites as promising sources of novel organic natural agents.

Objective: In the present study, 29 varieties of medicinal plants were screened for the presence of ADA inhibitors.