I/CFCOAg-mediated iodolactonization of various allenoic acids to access versatile 6- to 9-membered ring vinylic iodolactones.

Medium-sized lactones are important structural units, but their synthesis remains a great challenge. Herein, we report I/CFCOAg-mediated iodolactonization of allenoic acids to synthesize various 6- to 9-membered ring vinylic iodolactones in 16-89% yield. This protocol not only develops a new cyclization strategy of allenoic acids, but also provides highly functionalized medium-sized lactones containing alkene and halogen groups.

Synthesis of 4-aryl-3,4-dihydrocoumarins and 4-aryl-4-chromenes Er(OTf)-catalyzed cascade reactions of -quinone methides with 1,3-dicarbonyl compounds.

The Er(OTf)-catalyzed cascade cyclization reaction of -quinone methides (-QMs) with various 1,3-dicarbonyl compounds has been developed, which efficiently constructed a series of versatile 4-aryl-3,4-dihydrocoumarins and 4-aryl-4-chromenes. Herein, we not only propose a novel cyclization strategy of -QMs, but also provide an easy access to structurally diverse coumarins and chromenes.

[Quantitative determination of the beta-2-microglobulin monomer by gel filtration chromatography].

Beta-2-microglobulin (B2M) is an important material in dialysis-related amyloidosis research. Unfortunately, the quantitative detection of the B2M monomer is difficult during B2M production. In this study, we established a method for the detection of the B2M monomer and its dimer in solution via gel filtration chromatography.

Design, synthesis and biological evaluation of novel 3H-imidazole [4,5-b] pyridine derivatives as selective mTOR inhibitors.

A series of 3H-imidazo [4,5-b] pyridines derivatives were designed and synthesized as selective mTOR inhibitors. The systematic optimization of the molecules resulted in the identification of two compounds 10d and 10n with nanomolar mTOR inhibitory activity and selectivity over PI3Kα. Besides, compounds 10d and 10n demonstrated attractive potency against human breast cancer cells (MCF-7) and human ovarian cancer cell (A2780).

Optimization of dilution refolding conditions for a camelid single domain antibody against human beta-2-microglobulin.

Single domain antibody (sdAb) is often expressed as inclusion bodies in Escherichia coli cytoplasm. Establishing an effective in vitro refolding method for sdAb obtained from inclusion bodies would be important for sdAb research. In this study, dilution refolding condition for a camelid sdAb specific against human beta-2-microglobulin was optimized for the sdAb purified from the inclusion bodies of E.