Charge Relocation Enables a Modular and Diastereoselective Synthesis of cis-Substituted Tetrahydrofurans.

Diastereoselective construction of organic scaffolds from simple and commercial materials is a powerful strategy in contemporary organic synthesis. Herein, we report a novel disconnection for the direct preparation of tetrahydrofurans (THFs) and corresponding derivatives from acyl chlorides and alkenes using charge relocation. Newly synthesised Hantzsch ester derivatives, functioning both as hydride sources and selectivity modulators, enabled exceptional diastereoselectivity.

A Practical and Regioselective Strategy for Aromatic C-H Difunctionalization via Site-Selective C-H Thianthrenation.

Herein, we present a novel Catellani-type reaction that employed aryl-thianthrenium salts as aryl substrates to trigger the subsequent palladium/norbornene cooperatively catalyzed progress. This strategy can achieve site-selective C-H difunctionalization of aryl compounds without directing groups or a known initiating reagent. A series of functionalized syntheses of bioactive molecules further demonstrated the potential of this strategy.

Isolation, identification, and induced differentiation of satellite cells from skeletal muscle of adult tree shrews.

A method for the in vitro isolation, purification, identification, and induced differentiation of satellite cells from adult tree shrew skeletal muscle was established. The mixed enzyme digestion method and differential adhesion method were used to obtain skeletal muscle satellite cells, which were identified and induced to differentiate to verify their pluripotency. The use of a mixture of collagenase II, hyaluronidase IV, and DNase I is an efficient method for isolating adult tree shrew skeletal muscle satellite cells.

The regulation of expression and splicing of transcription factors are related to the muscle damage caused by radiation in tree shrews.

Radiotherapy-induced muscle injury (RIMI) is a major complication of radiotherapy for nasopharyngeal carcinoma. Transcription factor (TF) expression and alternative splicing are crucial events in transcriptional and posttranscriptional regulation, respectively, and are known to be involved in key signaling pathways contributing to a variety of human disorders, including radiation injury. To investigate the TFs and alternative splicing events involved in RIMI, we constructed a tree shrew model as described previously in which the RIMI group received 20 Gy of irradiation on the tensor veli palatini (TVP) muscles.

Integrative analyses of RNA-seq and ChIP-seq Reveal MITF as a Target Gene of TFPI-2 in MDA231 Cells.

Breast cancer is the most prevalent cancer in female patients worldwide. Tissue factor pathway inhibitor 2 (TFPI-2) is identified as an important tumor suppressor in various cancers. Recent studies have shown that TFPI-2 translocates into the nucleus, where it modulates the transcription of the matrix metalloproteinase-2 (MMP-2) gene.

C-H Hydroxyalkylation or Methylation of Aryl Iodides by Ethers and TMSI via a Catellani Strategy.

In this paper, in the presence of trimethylsilyl iodide, the direct -C-H hydroxyalkylation/methylation of aryl iodines was effectively realized via palladium/norbornene cooperative catalysis when low-cost tetrahydrofuran and 1,2-dimethoxyethane were used as alkyl sources. Heck, Suzuki, and Sonogashira coupling and hydrogenation were all compatible with the reaction as termination steps. In addition, neuromuscular agents and cardiovascular agents were synthesized in one step by this method, showing their potential application value.

Analysis of the clinical and genetic characteristics of a Chinese family with osteogenesis imperfecta type I.

Background: Osteogenesis imperfecta type I (OI-I) is a rare genetic disorder characterized by skeletal deformity, bone fragility, blue sclerae, dentinogenesis imperfecta, and hearing loss. The current study aimed to confirm the clinical diagnosis and genetic cause of OI-I in a four-generation Chinese family.

Methods: Clinical investigation and pedigree analysis were conducted to characterize the phenotypic manifestations of a Chinese family with OI-I.

Copper-Catalyzed Hydrogen Atom Transfer and Aryl Migration Strategy for the Arylalkylation of Activated Alkenes.

Herein, we describe the copper-catalyzed arylalkylation of activated alkenes via hydrogen-atom transfer and aryl migration strategy. The reaction was carried out through a radical-mediated continuous migration pathway using -fluorosulfonamides as the alkyl source. The primary, secondary, and tertiary alkyl radicals formed by intramolecular hydrogen-atom transfer proceeded smoothly.

Site-selective coupling of remote C(sp)-H/-C(sp)-H bonds enabled by Ru/photoredox dual catalysis and mechanistic studies.

Construction of C(sp)-C(sp) bonds regioselective coupling of C(sp)-H/C(sp)-H bonds is challenging due to the low reactivity and regioselectivity of C-H bonds. Here, a novel photoinduced Ru/photocatalyst-cocatalyzed regioselective cross-dehydrogenative coupling of dual remote C-H bonds, including inert γ-C(sp)-H bonds in amides and -C(sp)-H bonds in arenes, to construct -alkylated arenes has been accomplished. This metallaphotoredox-enabled site-selective coupling between remote inert C(sp)-H bonds and -C(sp)-H bonds is characterized by its unique site-selectivity, redox-neutral conditions, broad substrate scope and wide use of late-stage functionalization of bioactive molecules.

Three-Component Ru-Catalyzed Regioselective Alkylarylation of Vinylarenes via -Selective C(sp)-H Bond Functionalization.

We report a novel Ru-catalyzed regioselective alkylarylation of vinylarenes with alkyl halides and arenes via -C(sp)-H bond functionalization to construct 1,1-diarylalkanes that generally show bioactivity. In this transformation, a wide spectrum of primary, secondary, and tertiary alkyl halides and electronically varied arenes was well-tolerated. This reaction is characterized by its exquisite regioselectivity of vinylarenes, unique -C(sp)-H selectivity, and redox-neutral conditions.

An Investigation of the Mechanisms of Radiation-Induced Muscle Injury in a Tree Shrew () Model.

Background: Animal models suitable for investigating mechanisms behind radiation-induced muscle injury are lacking. We developed a tree shrew model of such injury and investigated pathological changes and mechanisms.

Methods: Animals were divided into control (n = 5), radiation-induced acute injury (n = 5), and radiation-induced chronic injury (n = 5) groups.

Analysis of the risk of death and clinical management for nasal or nasopharyngeal bleeding occurring after radiotherapy for nasopharyngeal carcinoma.

Objective: To retrospectively analyze the risk factors for death in patients with nasal or nasopharyngeal bleeding after radiotherapy for nasopharyngeal carcinoma, and to explore clinical management strategies for the disease.

Methods: This was a retrospective case-control study. The clinical data from patients diagnosed with nasopharyngeal or nasopharyngeal hemorrhage after radiotherapy for nasopharyngeal carcinoma at the First Affiliated Hospital of Guangxi Medical University between January 2006 and October 2021 were retrospectively analyzed.

Lewis-Acid-Catalyzed Tandem Cyclization by Ring Expansion of Tertiary Cycloalkanols with Propargyl Alcohols.

A new method for the efficient synthesis of hexahydro-1-fluorene and octahydrobenzo[]azulene derivatives through a ring-expansion strategy is reported. With an appropriate combination of thulium(III) trifluoromethanesulfonate and 13X molecular sieves, a range of unsaturated polycyclic compounds were obtained in good yields. Mechanism studies reveal that the reaction is more likely to undergo Meyer-Schuster rearrangement, ring expansion, and Friedel-Crafts-type pathways, which provide a conceptually different strategy for the ring opening of tertiary cycloalkanols.

Copper-Catalyzed Direct Allenylation of Inactive Cyclic Ethers.

We report here a direct allenylation reaction of inactive cyclic ethers. The reaction proceeds through a copper-catalyzed 1,4-difunctionalization of 1,3-enynes, with cyano group installed at the allenes simultaneously. This methodology shows a broad functional group compatibility to 1,3-enynes.

Highly regioselective and stereoselective synthesis of C-Aryl glycosides nickel-catalyzed -C-H glycosylation of 8-aminoquinoline benzamides.

C-Aryl glycosides are of high value as drug candidates. Here a novel and cost-effective nickel catalyzed ortho-CAr-H glycosylation reaction with high regioselectivity and excellent α-selectivity is described. This method shows great functional group compatibility with various glycosides, showing its synthetic potential.

Apatinib for the treatment of metastatic or locoregionally recurrent nasopharyngeal carcinoma after failure of chemotherapy: A multicenter, single-arm, prospective phase 2 study.

Background: The authors aimed to investigate the efficacy and safety of apatinib in patients with metastatic or locoregionally recurrent nasopharyngeal carcinoma (NPC).

Methods: A multicenter, single-arm, prospective phase 2 study was conducted on patients (18-70 years of age) with metastatic or recurrent NPC who had failed chemotherapy. Patients with recurrent disease involving vascular structure invasion were excluded.

A de novo mutation of the SOX10 gene associated with inner ear malformation in a Guangxi family with Waardenburg syndrome type II.

Objective: Waardenburg syndrome type 2 (WS2) is a rare neural-crest disorder, characterized by heterochromic irides or blue eyes and sensorineural hearing loss. The aim of this study was to analyze the clinical features and investigate the genetic cause of WS2 in a small family from Guangxi Zhuang Autonomous region.

Methods: Whole-exome sequencing and mutational analysis were used to identify disease-causing genes in this family.

Cu-Catalyzed Direct C-H Alkylation of Polyfluoroarenes via Remote C(sp)-H Functionalization in Carboxamides.

A novel dehydrogenative coupling reaction of -fluorocarboxamides with polyfluoroarenes forming C(sp)-C(sp) bonds enabled by copper catalysis has been accomplished. -Fluorocarboxamides are postulated to undergo copper-mediated dehydrogenative cross-coupling reaction with electron-deficient polyfluoroarenes via a radical pathway. Benzylic C-H bonds and aliphatic C-H bonds in -fluorocarboxamides could proceed smoothly and demonstrated excellent regioselectivity.

Formation of -Allyl- and Allenyl-Modified Amides via Intermolecular Claisen Rearrangement.

We developed a new transition-metal-free intermolecular Claisen rearrangement process to introduce allyl and allenyl groups into the α position of tertiary amides. In this transformation, amides were activated by trifluoromethanesulfonic anhydride to produce the keteniminium ion intermediates that exhibit strong electrophilic activity. This atom-economical process delivers α position-modified amides under mild conditions in moderate to good yields and showcases a broad substrate compatibility.

Gold-Catalyzed Tandem Annulations of Pyridylhomopropargylic Alcohols with Propargyl Alcohols.

A gold-catalyzed tandem annulation of propargylic alcohols and pyridylhomopropargylic alcohols is achieved, providing an atom-economical approach to a diverse set of polycyclic dihydrobenzofurans in good yields. The reaction proceeds via the 5- cyclization/Meyer-Schuster rearrangement/Friedel-Crafts-type pathway. In this way, three C-C bonds and one C-O bond form to give a polycyclic skeleton in a one-pot process.

Three-component ruthenium-catalyzed remote C-H functionalization of 8-aminoquinoline amides.

Multicomponent reactions can efficiently construct complex molecular structures from simple precursors. Herein, a novel ruthenium-catalyzed three-component highly selective remote C-H functionalization of 8-aminoquinoline amides has been described. The reaction tolerates a wide range of functional groups, producing arylation/difluoroalkylation products of olefins with potential biological activity and pharmaceutical value.

Identification and functional analysis of a novel missense mutation of PAX3 associated with Waardenburg syndrome type I.

Purpose: Waardenburg syndrome type 1 (WS1) is a rare genetic disorder characterized by dystopia canthorum, abnormal iris pigmentation, and congenital hearing loss with variable penetrance.WS1 is caused by mutations in paired box gene 3 (PAX3). The current study aimed to investigate the genetic cause of hearing loss in a four-generation Chinese WS1 family.

Organocatalyzed Synthesis of Functionalized Quinolines.

As one of the most widely investigated compound skeleton, quinolines possess important medicinal and biological activities. As such, a great number of literatures, including reviews, have reported various methodologies to construct quinolines. Recently, organocatalyzed reactions have attracted the attention of organic chemists due to its being "green" because the reactions avoid the use of toxic metals.

A novel ABHD12 nonsense variant in Usher syndrome type 3 family with genotype-phenotype spectrum review.

Usher syndrome (USH) is a clinically common autosomal recessive disorder characterized by retinitis pigmentosa (RP) and sensorineural hearing loss with or without vestibular dysfunction. In this study, we identified a Hunan family of Chinese descent with two affected members clinically diagnosed with Usher syndrome type 3 (USH3) displaying hearing, visual acuity, and olfactory decline. Whole-exome sequencing (WES) identified a nonsense variant in ABHD12 gene that was confirmed to be segregated in this family by Sanger sequencing and exhibited a recessive inheritance pattern.