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Bacterial wound infection has emerged as a pivotal threat to human health worldwide, and the situation has worsened owing to the gradual increase in antibiotic‐resistant bacteria caused by the improper use of antibiotics. To reduce the use of antibiotics and avoid the increase in antibiotic‐resistant bacteria, researchers are increasingly paying attention to photodynamic therapy, which uses light to produce reactive oxygen species to kill bacteria. Treating bacteria‐infected wounds by photodynamic therapy requires fixing the photosensitizer (PS) at the wound site and maintaining a certain level of wound humidity. Hydrogels are materials with a high water content and are well suited for fixing PSs at wound sites for antibacterial photodynamic therapy. Therefore, hydrogels are often loaded with PSs for treating bacteria‐infected wounds via antibacterial photodynamic therapy. In this review, we systematically summarised the antibacterial mechanisms and applications of PS‐loaded hydrogels for treating bacteria‐infected wounds via photodynamic therapy. In addition, the recent studies and the research status progresses of novel antibacterial hydrogels are discussed. Finally, the challenges and future prospects of PS‐loaded hydrogels are reviewed. [ABSTRACT FROM AUTHOR]

Background: Postoperative anastomotic leakage (PAL) is a serious complication of gastric cancer surgery. Although perioperative management has made considerable progress, anastomotic leakage (AL) cannot always be avoided. The purpose of this study is to evaluate whether intraoperative leak testing (IOLT) can reduce the incidence of PAL and other postoperative outcomes in gastric cancer surgery. Materials and methods: In this meta-analysis, we searched the PubMed, Embase, and Cochrane Library databases for clinical trials to assess the application of IOLT in gastric cancer surgery. All patients underwent laparoscopic radical gastrectomy for gastric cancer surgery. Studies comparing the postoperative outcomes of IOLT and no intraoperative leak testing (NIOLT) were included. Quality assessment, heterogeneity, risk of bias, and the level of evidence of the included studies were evaluated. PAL, anastomotic-related complications, 30-day mortality, and reoperation rates were compared between the IOLT and NIOLT group. Results: Our literature search returned 721 results, from which six trials (a total of 1,666 patients) were included in our meta-analysis. Statistical heterogeneity was low. The primary outcome was PAL. IOLT reduced the incidence of PAL [2.09% vs 6.68%; (RR = 0.31, 95% Cl 0.19–0.53, P < 0.0001]. Anastomotic-related complications, which included bleeding, leakage, and stricture, were significantly higher in the NIOLT group than in the IOLT group [3.24% VS 10.85%; RR = 0.30, 95% Cl 0.18–0.53, P < 0.0001]. Moreover, IOLT was associated with lower reoperation rates [0.94% vs 6.83%; RR = 0.18, 95% CI 0.07–0.43, P = 0.0002]. Conclusion: Considering the observed lower incidence of postoperative anastomotic leakage (PAL), anastomotic-related complications, and reoperation rates, IOLT appears to be a promising option for gastric cancer surgery. It warrants further study before potential inclusion in future clinical guidelines. [ABSTRACT FROM AUTHOR]

Abstract: A three-component reaction based on trapping of ammonium ylides with formaldehyde was first reported. This reaction offers a new strategy for the synthesis of α-aryl serine derivatives and can be extended to the preparation of α-aryl threonine derivatives. Synthetic application of the three component reaction for the preparation of hydroquinoxaline derivative was also demonstrated. [Copyright &y& Elsevier]

Both isoindolinones and continuous quaternary carbons play important roles in pharmaceutical scaffolds. However, few examples have been developed to construct isoindolinones containing continuous quaternary carbons due to the steric hindrance effect. Here, a rhodium(II)-catalyzed reaction of 3-hydroxyisoindolinones and diazos via an intermolecular OH transfer to deliver the isoindolinone derivatives containing continuous quaternary carbons as products is developed in high yields of up to 89% via an intermolecular OH transfer with a green chemistry metric E-factor of 5.70. The resulting products exhibit antiviral activity against SARS-CoV-2 3CL protease (3CLpro) and control investigations show that the quaternary carbons and hydroxyl group are essential for the bioactivity. [ABSTRACT FROM AUTHOR]

Aim: To compare the blood glucose control of patients with type 2 diabetes mellitus (T2DM) with different treatment methods, oral hypoglycemic agents (OHA) monotherapy, insulin injection and combined therapy (OHA + insulin injection) and evaluate their satisfaction with the medical care. Methods: A total of 1512 T2DM patients were assessed, to compare the effects of different treatment methods on glycemic control in T2DM patients, the influencing factors of patients' satisfaction with medical care measures and their relationship with glycemic control. Fasting plasma glucose (FPG), 2 hrs postprandial plasma glucose (2hPG) and HbA1c were measured as the standard of the glycemic control. Satisfaction was defined using the simplified version of DAWN of chronic disease care patient scale (PACIC - DSF). Results: In this study, the FPG compliance rate, 2hPG compliance rate and HbA1c compliance rate were 25.5%, 22.7% and 19.5%, respectively. The differences in the glycemic control compliance rates of different treatment methods were not statistically significant. The total score of PACIC - DSF was 34.54±11.65(p>0.05), and the influencing factors included fast blood glucose (FBG) and 2hPG, 2hPG and PACIC - DSF were negatively correlated. Conclusions: The T2DM glycemic control rate in China is currently low. From the score of the PACIC - DSF, there is no significant difference in general satisfaction with medical care measures in different treatments. What is more, education level, occupation and exercise of patients with type 2 diabetes had influence on PACIC - DSF score. Different treatment methods have no influence on the glycemic control of patients with T2DM. FPG value and the 2hPG value are negative correlation with the satisfaction of patients in medical care measures. [ABSTRACT FROM AUTHOR]

The article presents chemical equations related to the article on the synthesis of Aryl Serine derivatives by C. Wang and colleagues, published in the "Tetrahedron" in 2013.

The article mentions the advancement of chiral bronsted acids as cooperative catalysts for multicomponent and cascade reactions, published in the 2013 issue of "Asian Journal of Organic Chemistry."

A Rh(II)/boron reagent co-catalyzed unprecedent transformation was established for the rapid construction of multi-substituted conjugated dienones under mild conditions by trapping allene carbocations with oxonium ylides from simple starting points in yields up to 85%. Two C＝C double bonds, one C–C and one C–O single bond were built in this one-pot reaction. The diversity-oriented strategy was also established to synthesize alkyne ether and dihydrofuran derivatives by a substrate-depended fashion. [ABSTRACT FROM AUTHOR]

Chemotherapy combining with surgical treatment has been the main strategy for osteosarcoma treatment in clinical. Due to unclear pathogenesis and unidentified drug targets, significant progress has not been made in the development of targeted drugs for osteosarcoma during the past 50 years. Our previous discovery reported compound R - 8i with a high potency for the treatment of osteosarcoma by phenotypic screening. However, both the metabolic stability and bioavailability of R - 8i are poor (T 1/2 = 5.36 min, mouse liver microsome; and bioavailability in vivo F = 52.1 %, intraperitoneal administration) which limits it use for further drug development. Here, we described an extensive structure−activity relationship study of thiazolidine-4-one sulfone inhibitors from R - 8i , which led to the discovery of compound 68. Compound 68 had a potent cellular activity with an IC 50 value of 0.217 μM, much higher half-life (T 1/2 = 73.8 min, mouse liver microsome) and an excellent pharmacokinetic profile (in vivo bioavailability F = 115 %, intraperitoneal administration). Compound 68 also showed good antitumor effects and low toxicity in a xenograft model (44.6 % inhibition osteosarcoma growth in BALB/c mice). These results suggest that compound 68 is a potential drug candidate for the treatment of osteosarcoma. [Display omitted] • Discovering lead compound 68 from the metabolites for anti-osteosarcoma. • 68 shows an obviously improved metabolic stability with 115 % bioavailability in vivo. • Compound 68 possesses 44.6 % inhibition osteosarcoma growth and low toxicity in mice. • Compound 68 significantly suppresses osteosarcoma cell migration in vitro. [ABSTRACT FROM AUTHOR]

The coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has posed a serious threat to human. Since there are still no effective treatment options against the new emerging variants of SARS-CoV-2, it is necessary to devote a continuous endeavor for more targeted drugs and the preparation for the next pandemic. Salvia miltiorrhiza and its active ingredients possess wide antiviral activities, including against SARS-CoV-2. Danshensu, as one of the most important active ingredients in Salvia miltiorrhiza , has been reported to inhibit the entry of SARS-CoV-2 into ACE2 (angiotensin-converting enzyme 2)-overexpressed HEK-293T cells and Vero-E6 cells. However, there is a paucity of information regarding its detailed target and mechanism against SARS-CoV-2. Here, we present Danshensu as a covalent inhibitor of 3-chymotrypsin-like protease (3CLpro) against SARS-CoV-2 by the time-dependent inhibition assay (TDI) and mass spectrometry analysis. Further molecular docking, site-directed mutagenesis, circular dichroism (CD) and fluorescence spectra revealed that Danshensu covalently binds to C145 of SARS-CoV-2 3CLpro, meanwhile forming the hydrogen bonds with S144, H163 and E166 in the S1 site. Structure-based optimization of Danshensu led to the discovery of the promising compounds with good inhibitory activity and microsomal stability in vitro. Due to Danshensu inhibiting lung inflammation in the mouse model, we found that Danshensu derivatives also showed better anti-inflammatory activity than Danshensu in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells. Thus, our study provides not only the clue of the efficacy of Salvia miltiorrhiza against SARS-CoV-2, but also a detailed mechanistic insight into the covalent mode of action of Danshensu for design of covalent inhibitors against SARS-CoV-2 3CLpro, highlighting its potential as a bifunctional molecule with antivirus and anti-inflammation. • Potential target of Danshensu with anti-SARS-CoV-2 activity is discussed. • Danshensu was confirmed to covalently bind to C145 of SARS-CoV-2 3CLpro, meanwhile forming the hydrogen bonds with S144, H163 and E166 in the S1 site. • Structure-based optimization of Danshensu led to the discovery of the promising bifunctional molecules with antivirus and anti-inflammation. [ABSTRACT FROM AUTHOR]

Trapped: A Michael‐aldol‐type cascade reaction including the trapping of an oxonium ylide through a delayed proton shift leads to the formation of multiple stereocenters in a mild one‐pot synthesis. Enantiomerically pure indanol derivatives with four stereocenters and a stereogenic quaternary carbon center were easily obtained through this method in moderate to good yields. [ABSTRACT FROM AUTHOR]

Abgefangen: Eine Michael ‐ Aldol ‐ artige Kaskadenreaktion, in der ein Oxoniumylid durch einen verzögerten Protonenshift abgefangen wird, führt zur Bildung mehrerer Stereozentren in einer milden Eintopfsynthese. Mit dieser Methode wurden enantiomerenreine Indanolderivate mit vier Stereozentren und einem stereogenen quartären Stereozentrum in moderaten bis guten Ausbeuten erhalten. [ABSTRACT FROM AUTHOR]

Neonatal hypoxic-ischemic encephalopathy (HIE) is one of the main causes of death and nervous system damage in neonates. The aim of the present study was to investigate the effect of the Toll-like receptor 4 (TLR4) antagonist TAK-242 on HIE. The Rice-Vannucci method was used for ligation of the left common carotid artery, followed by hypoxic treatment for 2.5 h to establish a neonatal HIE rat model. Rats were intraperitoneally injected with 7.5 ml/kg TAK-242 after hypoxia-ischemia. It was demonstrated that TAK-242 significantly reduced the infarct volume and cerebral edema content of neonatal rats after HIE, alleviating neuronal damage and neurobehavioral function deficits. Furthermore, TAK-242 decreased the protein expression levels of TLR4, MyD88, TIR-domain-containing adapter-inducing interferon-β (TRIF), NF-κB, tumor necrosis factor α (TNF-α) and interleukin-1β in the hippocampus. The present results suggested that TAK-242 may exert a neuroprotective effect after HIE by inhibiting the TLR4/MyD88/TRIF/NF-κB signaling pathway, and reducing the release of downstream inflammatory cytokines. [ABSTRACT FROM AUTHOR]

A highly enantioselective trapping of protic phosphoramidate ammonium ylides with α-imino esters is reported. The intriguing Rh2(OAc)4 and chiral Brønsted acid co-catalyzed three-component Mannich-type reaction of a diazo compound, a phosphoramidate, and an α-imino ester provides a rapid and efficient access to 2,3-diaminosuccinic acid derivatives with a high level control of diastereo- and enantioselectivity. [ABSTRACT FROM AUTHOR]

An enantioselective four-component reaction of a diazoketone, water, an aniline and ethyl glyoxylate in the presence of catalytic Rh2(OAc)4 and a chiral Brønsted acid was developed to efficiently produce β-hydroxy-α-amino acid derivatives in good yields with high diastereoselectivity and enantioselectivity. [ABSTRACT FROM AUTHOR]

A formal carbene insertion into C O double bonds of 2-hydroxycinnamaldehydes catalyzed by Rh 2 (esp) 2 with Na 2 CO 3 as additive has been disclosed by using aryldiazoacetates as carbene precursors. 2 H -chromenes with a quaternary carbon at C-2 position were readily obtained from simple starting materials in good yields with excellent diastereoselectivity under mild reaction conditions in one pot. The reaction mechanism was investigated and proposed as the formation of epoxide intermediate from Rh(II)-associated carbene and ( E )-2-hydroxycinnamaldehyde and followed by a cascade epoxide ring-opening procedure in which the ( E )-intermediate was converted into the ( Z )-intermediate to give ( Z )-products. [ABSTRACT FROM AUTHOR]

1,2,5-Triol derivatives with vicinal chiral centers have been synthesized from simple starting materials by one-pot method in good yields and with an excellent enantioselectivity. This process was promoted by a chiral secondary amine and iridium(I) cocatalyzed three-component reaction of aryldiazoacetates and alcohols with enals as electrophiles followed by a reduction with NaBH4. Iridium(I)-associated oxonium ylide intermediates were efficiently generated and successfully trapped by the amine-activated enals via a selective 1,4-addition manner, generating enantioselective three-component coupling products. [ABSTRACT FROM AUTHOR]

Protein tyrosine phosphatase 1B (PTP1B) has been proposed to be an ideal target for treatment of type II diabetes and obesity. However, no druggable PTP1B inhibitor has been established and there is still an urgent demand for the development of structurally novel PTPIB inhibitor. Herein, we reported core-structurally novel PTP1B inhibitors with low micromole-ranged inhibitory activity by one-pot reaction from simple starting materials. Further studies demonstrated some of these active compounds had a specific selectivity over other PTPs. The structure and activity relationship was also described. The best active and selective compound 5e inhibited PTP1B activity with an IC 50 of 4.53 μM. Molecular docking analysis further demonstrated that compound 5e bound to the active pocket of PTP1B. The results might provide some insights for further development of new drugs for type II diabetes and obesity. [ABSTRACT FROM AUTHOR]

A transformation of cyclopropyl carbene generated from 2-cyclopropyl-2-diazoacetate via oxonium ylide was found by trapping the resulting ylide with imine. The asymmetric three-component reaction of cycloproyl diazoacetates, benzenemethanols and imines afforded a rapid and efficient method to synthesize complex cyclopropane derivatives with excellent diastereoselectivity and enantioselectivity. [ABSTRACT FROM AUTHOR]

A one-pot synthesis of new oxindole-fused polycyclic scaffolds is reported. The process involves a three-component [3+2] cycloaddition followed by cyclization through an intramolecular Michael addition. The reaction gives easy access to oxindole-fused spirotetrahydrofurochromans in moderate to good yields with high regio- and diastereoselectivity. These compounds could be useful for for drug discovery. Further modification was achieved by reduction of the nitro group, and intramolecular amide formation to give the corresponding lactams. The resulting heterocyclic products show good inhibitory activity against the enzyme PTP1B in vitro. [ABSTRACT FROM AUTHOR]

The first example of chiral secondary amine and iridium(i) co-catalyzed enantioselective three-component reaction of aryldiazoacetates, indoles and enals was rationally designed and developed to afford 3-substituted indole derivatives in good yields and with moderate diastereoselectivity as well as excellent enantioselectivity. This reaction is proposed to proceed through the enantioselective trapping of iridium(i)-associated zwitterionic intermediates via selective 1,4-addtition to the chiral amine activated enals. [ABSTRACT FROM AUTHOR]

The chiral RhI-diene-catalyzed asymmetric three-component reaction of aryldiazoacetates, aromatic amines, and β-nitroacrylates was achieved to obtain γ-nitro-α-amino-succinates in good yields and with high diastereo- and enantioselectivity. This reaction is proposed to proceed through the enantioselective trapping of RhI-associated ammonium ylides by nitroacrylates. This new transformation represents the first example of RhI-carbene-induced ylide transformation. [ABSTRACT FROM AUTHOR]

The chiral RhI-diene-catalyzed asymmetric three-component reaction of aryldiazoacetates, aromatic amines, and β-nitroacrylates was achieved to obtain γ-nitro-α-amino-succinates in good yields and with high diastereo- and enantioselectivity. This reaction is proposed to proceed through the enantioselective trapping of RhI-associated ammonium ylides by nitroacrylates. This new transformation represents the first example of RhI-carbene-induced ylide transformation. [ABSTRACT FROM AUTHOR]

An efficient one-pot two-step synthetic strategy to access highly selective N 2-substituted-1,2,3-triazole from aryl ethynylenes, azides and furan has been developed via a radical transformation. 17 examples of aryl ethynylene with various substituents were converted into their corresponding functionalized N 2-substituted-1,2,3-triazole derivatives in good yields. [Display omitted] [ABSTRACT FROM AUTHOR]

The rhodium acetate and chiral Broensted acid co-catalyzed three-component Mannich-type reaction of a diazo compound (I), a phosphoramidite (II), and an α-imino ester (III) provides an efficient access to title compounds (IV) with high levels of diastereo- and enantioselectivity. [ABSTRACT FROM AUTHOR]

Highly chemoselective and enantioselective one-pot reactions involved in the oxidative functionalization of Csp3–H bonds adjacent to nitrogen atoms in N-aryl glycine esters were developed. The method provided rapid access to a variety of highly functionalized β-hydroxyl-α-amino acid derivatives from simple starting materials under mild conditions. [ABSTRACT FROM AUTHOR]

Abstract: Three-component reactions of aryl diazoacetates, arylamines and N-sulfonyl aldimines cooperatively catalyzed by squaramides and dirhodium acetate are reported to afford N-sulfonyl α,β-diamino acid derivatives in moderate to good yields and diastereoselectivity. [Copyright &y& Elsevier]

An elegant synergistic catalytic system comprising a ruthenium complex with a chiral Brønsted acid was developed for a four-component Mannich/cascade aza-Michael reaction. The ruthenium-associated ammonium ylides successfully trapped with in situ generated imines indicates a stepwise process of proton transfer in the ruthenium-catalyzed carbenoid NH insertion reaction. The different decomposition abilities of various ruthenium complexes towards diazo compounds were well explained by the calculated thermodynamic data. The transformation features a mild, rapid, and efficient method for the synthesis of enantiomerically pure 1,3,4-tetrasubstituted tetrahydroquinolines bearing a quaternary stereogenic carbon center from simple starting precursors in moderate yields with high diastereo- and enantioselectivity. [ABSTRACT FROM AUTHOR]

An iron porphyrin-catalyzed three-component reaction of ethyl diazoacetate with aliphatic amines and β,γ-unsaturated α-keto esters is reported. The use of iron porphyrin catalyst allows aliphatic amines to be used as the substrate without encountering catalyst poisoning issue and a series of β-hydroxy-α-amino esters are produced in high yields with excellent regioselectivities. [ABSTRACT FROM AUTHOR]

Due to unknown pathogenesis and unidentified drug target, no drug for the treatment of osteosarcoma (OS) has been launched to the market. Herein, thiazolidinone 1a was discovered as a hit compound by phenotypic screening with an in-house patrimonial collection of structural diversity. The following SAR (Structure-Activity Relationship) study affords the final water-soluble lead compound (R)- 8i as a potential inhibitor for the proliferation of OS cells by the modulation of solubility of the compounds with remarkable cellular potency (IC 50 = 21.9 nM for MNNG/HOS cells) and in vivo efficacy (52.9% inhibition OS growth in mice), as well as pharmacokinetic properties. (R)- 8i also significantly suppresses OS cell migration in vitro and showed to be well-tolerated. Our preliminary investigation shows that the effects of (R)- 8i are not dependent on p53 and myoferlin (MYOF). These results suggest that (R)- 8i might be a potential drug candidate for OS treatment. [Display omitted] • Thiazolidinones were discovered for treating osteosarcoma by phenotypic screening. • The screening used an in-house patrimonial collection of structural diversity. • Lead compound (R)- 8i selectively inhibit osteosarcoma cell in vitro and in vivo. • (R)- 8i also significantly suppresses osteosarcoma cell migration in vitro. • (R)- 8i presents a considerable bioavailability and a low toxicity. [ABSTRACT FROM AUTHOR]

The article presents information on a chemical reaction for construction of chiral hydroxy-amino acid derivatives.

This is the first Rh(II)-catalyzed intramolecular three-component cascade Michael-aldol-type reaction yielding 1-indanol compounds. [ABSTRACT FROM AUTHOR]

Au-Fe3O4 nanoparticles were widely used as nanoplatforms for biologic applications through readily further functionalization. Dopamine (DA)-coated superparamagnetic iron oxide (SPIO) nanoparticles (DA@Fe3O4) have been successfully synthesized using a one-step process by modified coprecipitation method. Then 2-3 nm gold nanoparticles were easily conjugated to DA@Fe3O4 nanoparticles by the electrostatic force between gold nanoparticles and amino groups of dopamine to afford water-soluble Au-Fe3O4 hybrid nanoparticles. A detailed investigation by dynamic light scatting (DLS), transmission electron microscopy (TEM), fourier transform infrared (FT-IR) and X-ray diffraction (XRD) were performed in order to characterize the physicochemical properties of the hybrid nanoparticles. The hybrid nanoparticles were easily functionalized with a targeted small peptide A54 (AGKGTPSLETTP) and fluorescence probe fluorescein isothiocyanate (FITC) for liver cancer cell BEL-7402 imaging. This simple approach to prepare hybrid nanoparticles provides a facile nanoplatform for muti-functional derivations and may be extended to the immobilization of other metals or bimolecular on SPIO surface. [ABSTRACT FROM AUTHOR]

The effect of the pH value of gold ion plating (PCG) solution on the growth of gold nanoshells with about 100-nm silica cores and 15-nm gold shells was systematically investigated by dynamic light scattering, UV-Vis spectroscopy, scanning electron microscopy, and transmission electron microscopy. The results showed that in PCG solutions, the rapid formation of monomers which intensively influenced by the reducibility of formaldehyde contributed to the growth of gold nanoshells. The reducibility of formaldehyde increased following the increasing pH value from 4.70 to 11.71. Thus at high pH value, it was easy to fabricate the complete gold nanoshells (except of the Cannizzaro reaction of formaldehyde at high pH value). Furthermore, we found that chloride ions also influenced the surface morphology of gold nanoshells by Ostwald ripening process through the Au-Cl complex. [ABSTRACT FROM AUTHOR]

Abstract: This research is aimed to develop a nanomicelle delivery system in order to enhance the solubility and stability of camptothecin (CPT) in aqueous media. In this case, α,β-poly[(N-carboxybutyl)-l-aspartamide] (PBAsp)–CPT was conjugated by the esterification between PBAsp and 20-OH of CPT, and hence used to fabricate nanomicelles with a particle size between the pore size of blood capillary in normal tissue and that in tumor tissue. It was worthy of note that the drug-loaded system of PBAsp–CPT nanomicelle improved the solubility and stability of CPT in aqueous media. However, with an increase of the CPT loading in PBAsp–CPT, the solubility sharply decreased. Meanwhile, the sizes of PBAsp–CPT nanomicelles showed a tendency of increase. Moreover, the drug release of PBAsp–CPT nanomicelles displayed a linear sustaining profile, and hence resulted in the essential decrease of cytotoxicity to L929 cell line. The assembled nanomicelles based on the PBAsp–CPT conjugates showed a great potential as polymer prodrug of tumor therapy, and the controlled nano-scale might achieve the passive tumor targeting. [Copyright &y& Elsevier]

Abstract: To design peptide-targeted iron oxide as magnetic resonance imaging (MRI) contrast agents, amino-functionalized magnetic nanogels were prepared by using N-(2-aminoethyl) methacrylamide hydrochloride (AEM·HCl) as monomer via new photochemical approach. Their chemical structure and composition were characterized by Fourier transform infrared spectra (FTIR) and thermogravimetric analyses (TGA). The core–shell structure of magnetic nanogels was confirmed by high-resolution transmission electron microscopy (HRTEM). The good storage stability, high magnetic content (88.7%), high saturation magnetizations and superparamagnetic behavior suggested their great potentials as MRI contrast agents, which were confirmed by their measurements of r 2 and coronal image of the crossing of mouse kidney. [Copyright &y& Elsevier]

Abstract: The aim of research is to develop and optimize delivery system for cis-dichlorodiammine platinum(II) (CDDP) based on polymer–metal complex nanomicelles with controllable particle size in order to achieve the passive tumor targeting. In particular, graft copolymers, mPEG–g-α,β-poly [(N-amino acidyl)-dl-aspartamide] (mPEG–g-PAAsp) were synthesized by the ring-opening reaction of polysuccinimide with mPEG-NH2 (M w: 2000 and 5000Da), and then with l-aspartic acid and l-glutamic acid, respectively. mPEG–g-PAAsp–CDDP complex nanomicelles were fabricated from mPEG–g-PAAsp and CDDP. The formation of mPEG–g-PAAsp–CDDP nanomicelles was confirmed by fluorescence spectrophotoscopy, electrical conductivity and particle size measurements. It was found that all the nanomicelles showed spherical shapes with clear core-shell structures and narrow size distributions. Their sizes ranged from 80 to 160nm, suggesting of their passive targeting potential to tumor tissue. With the increase of the molecular weight of mPEG, the sizes of mPEG–g-PAAsp–CDDP micelles showed a tendency to increase. mPEG–g-PAAsp–CDDP nanomicelles showed linear gradual drug release profiles in 40h, suggestion of their sustained drug release behaviors. Compared with CDDP, mPEG–g-PAAsp–CDDP micelles showed essential decreased cytotoxicity to Bel-7402 cell line. [Copyright &y& Elsevier]

A one-pot synthesis of new oxindole-fused polycyclic scaffolds is reported. [ABSTRACT FROM AUTHOR]

The article presents chemical equations related to the article "A Transformation of Cyclopropyl Carbene: A Highly Enantioselective Three-Component Reaction via Trapping Oxonium Ylide by Imine" by Mingfeng Li and others, published in the journal "Tetrahedron" in 2016.

The first example of chiral secondary amine and iridium(I) co-catalyzed enantioselective three-component reaction of aryldiazoacetates, indoles and enals is developed to afford 3-substituted indole derivatives in good yields and with moderate diastereoselectivity as well as excellent enantioselectivity. [ABSTRACT FROM AUTHOR]

An abstract of the article "An Ylide Transformation of Rhodium(I) Carbene: Enantioselective Three-Component Reaction Through Trapping of Rhodium(I)-Associated Ammonium Ylides by Β-Nitroacrylates" by Xiaochu Ma and colleagues is presented.

The title compounds show inhibitory activity on PTP1B and SIRT1 enzymes in vitro. [ABSTRACT FROM AUTHOR]

A four-component Mannich/cascade aza-Michael reaction using a ruthenium complex with a chiral Broensted acid is developed. [ABSTRACT FROM AUTHOR]

Ammonium ylides generated in situ from aryldiazo acetates and arylamines undergo Mannich-type reaction with N-sulfonyl aldimines to produce α,β-diamino acid derivatives. [ABSTRACT FROM AUTHOR]

The structure of the product (IVd) is confirmed by X-ray analysis. [ABSTRACT FROM AUTHOR]

The article presents chemical equations related to the article "Efficient Synthesis of Chiral Cyclic Acetals by Metal and Broensted Acid Co-Catalyzed Enantioselective Four-Component Cascade Reactions" by X. Guo and others published in the journal "Chemical Communications" in the 2014 issue.