CTPAD: an interactive web application for comprehensive transcriptomic profiling in allergic diseases.

Background: Allergic diseases are systemic chronic inflammatory diseases associated with multiorgan damage and complex pathogenesis. Several studies have revealed the association of gene expression abnormalities with the development of allergic diseases, but the biomedical field still lacks a public platform for comprehensive analysis and visualization of transcriptomic data of allergic diseases.

Objective: The aim of the study is to provide a comprehensive web tool for multiple analysis in allergic diseases.

Redox-Inducible Radiomimetic Photosensitizers Selectively Suppress Cancer Cell Proliferation by Damaging DNA through Radical Cation Chemistry.

Radiotherapy leverages ionizing radiation to kill cancer cells through direct and indirect effects, and direct effects are considered to play an equal or greater role. Several photosensitizers have been developed to mimic the direct effects of radiotherapy, generating radical cations in DNA models, but none has been applied in cellular studies. Here, we design a radiomimetic photosensitizer, producing DNA radical cations in cells for the first time.

Glutathione-dependent degradation of SMARCA2/4 for targeted lung cancer therapy with improved selectivity.

SMARCA2 and SMARCA4 are the mutually exclusive catalytic subunits of the mammalian Switch/Sucrose Non-Fermentable (SWI/SNF) chromatin remodeling complex, and have recently been considered as attractive synthetic lethal targets for PROTAC-based cancer therapy. However, the potential off-tissue toxicity towards normal tissues remains a concern. Here, we optimize a GSH-inducible SMARCA2/4-based PROTAC precursor with selective antitumor activity towards lung cancer cells and negligible cytotoxicity towards normal cells in both in vitro and in vivo studies.

Synthesis of -CF Amidines/Imidates/Thioimidates -CF Nitrilium Ions.

An efficient methodology for the synthesis of a wide range of -CF imidic acid derivatives is presented. In this reaction, -CF nitrilium ions were generated -trifluoromethylation of nitriles using PhICFCl under catalysis with DMAP, followed by the capture of N-, O-, or S-centered nucleophiles to give diverse -CF amidines, imidates, and thioimidates. The method provides a platform for preparing -CF compounds with potential applications.

ZnI-Catalyzed Aminotrifluoromethylation Cyclization of Alkenes Using PhICFCl.

We report here an alternatively catalytic aminotrifluoromethylation of alkenes using PhICFCl as a bifunctional reagent along with ZnI as a dual catalyst. A combined catalytic strategy was established for the intramolecular aminotrifluoromethylation of 4-pentenamines. As a result, a set of 2-trifluoroethyl-pyrrolidines was obtained in a high selectivity.

Trifluoromethylations of Alkenes Using PhICFCl as Bifunctional Reagent.

We described a trifluoromethylation of alkenes using PhICFCl as bifunctional reagent. Chlorotrifluoromethylated products were obtained when nonconjugated alkenes were treated with PhICFCl in 1,4-dioxane at 60 °C, while vinyl C-H trifluoromethylated products were obtained by further elimination of hydrochloride in the case of those conjugated alkene substrates in DMF. Broad substrate scope, especially including complex alkenes bearing biological active motifs, suggests that this mild reaction is feasible for late-stage modification in drug discovery.

Catalyst-free and selective trifluoromethylative cyclization of acryloanilides using PhICFCl.

Trifluoromethylation-triggered cyclization of alkenes provides a useful route to CF3-containing cyclic compounds. Current approaches to generate CF3-based initiators from a CF3 source require a catalyst or an activator. This work describes a catalyst-free protocol to innately produce electrophilic CF3 species from PhICF3Cl for trifluoromethylative cyclization of acryloanilides.

A direct catalytic ring expansion approach to o-fluoronaphthols and o/p-fluorophenols from indanones and 2-cyclopentenones.

A direct method for the synthesis of o-fluoronaphthols and o/p-fluorophenols has been developed by a catalytic ring expansion of indanones and 2-cyclopentenones, in which TMSCF2Br was used as a unique :CF2 source, a TMS transfer agent, as well as the Br(-) and F(-) releaser for the enolization, difluorocyclopropanation, desilylation, ring opening, defluorination, and aromatization sequence.