Design, synthesis and biological evaluation of novel dualaction statin conjugates with triglyceride and cholesterol lowering activities.

A series of novel dual-action statin conjugates, which exhibit both triglyceride and cholesterol lowering activities, have been systematically designed, synthesized, and subjected to comprehensive pharmacological evaluation. All the target compounds were characterized by HNMR, CNMR, and HRMS. Biological evaluation demonstrated that the majority of the synthesized compounds exhibited significant lipid-lowering and cholesterol-reducing activities.

Copper-mediated cascade radical cyclization of olefins with naphthalenyl iododifluoromethyl ketones.

Copper-mediated radical cyclization of naphthalenyl iododifluoromethyl ketones with olefins was successfully developed to generate a series of unprecedented gem-difluorodihydrophenanthrenones, especially 2,2-difluoro-3,4-dihydrophenanthren-1(2H)-one derivatives. This strategy features the use of cheap copper powder and excellent regioselectivity and diastereoselectivity, thus providing a facile approach for application in drug discovery and development. Preliminary mechanistic studies indicate the involvement of difluorinated radical intermediates.

Discovery of novel acylhydrazone neuraminidase inhibitors.

Neuraminidase (NA) plays a crucial role in the replication and transmission of influenza virus. NA inhibitors have been developed as effective treatments for influenza A and B infections. In this paper, a new lead neuraminidase inhibitor 6a (IC = 7.

Molecular modeling study, synthesis and biological evaluation of combretastatin A-4 analogues as anticancer agents and tubulin inhibitors.

As the major structural component of microtubules, tubulin is an interesting target for the development of anticancer agents. In this study, 64 tubulin polymerization inhibitors of five-membered heterocycle-based combretastatin A-4 analogues were studied by a combination of molecular modeling techniques including 3D-QSAR, molecular docking, and molecular dynamics (MD) simulation. The CoMFA (comparative molecular field analysis) and CoMSIA (comparative molecular similarity indices analysis) models were established with desirable statistical parameters and excellent predictive ability.

Suppression of Elp2 prevents renal fibrosis and inflammation induced by unilateral ureter obstruction (UUO) via inactivating Stat3-regulated TGF-β1 and NF-κB pathways.

Renal fibrosis and inflammation are common underlying processes of progressive kidney diseases. Elongator protein 2 (Elp2), identical to signal transducer and activator of transcription-3 (STAT-3)-interacting protein-1 (Stip1), is a component of the Elongator complex that regulates RNA polymerase II. Elp2 regulates STAT-3 activation to control various cellular processes.

Molecular modeling study of CP-690550 derivatives as JAK3 kinase inhibitors through combined 3D-QSAR, molecular docking, and dynamics simulation techniques.

To develop more potent JAK3 kinase inhibitors, a series of CP-690550 derivatives were investigated using combined molecular modeling techniques, such as 3D-QSAR, molecular docking and molecular dynamics (MD). The leave-one-out correlation (q) and non-cross-validated correlation coefficient (r) of the best CoMFA model are 0.715 and 0.

Combretastatin A-4 and Derivatives: Potential Fungicides Targeting Fungal Tubulin.

Combretastatin A-4, first isolated from the African willow tree Combretum caffrum, is a tubulin polymerization inhibitor in medicine. It was first postulated as a potential fungicide targeting fungal tubulin for plant disease control in this study. Combretastatin A-4 and its derivatives were synthesized and tested against Rhizoctonia solani and Pyricularia oryzae.

Effects of Patient-Controlled Epidural Analgesia and Patient-Controlled Intravenous Analgesia on Analgesia in Patients Undergoing Spinal Fusion Surgery.

We compared the outcomes of patient-controlled epidural analgesia (PCEA) and patient-controlled intravenous analgesia (PCIA) in analgesia after spinal fusion surgery. A total of 120 patients who underwent spinal fusion surgeries between April 2013 and April 2015 at Shaanxi Provincial People's Hospital were selected for this study based on defined inclusion criteria. All patients were randomly divided into 2 groups before surgery: PCEA group (n = 65) and PCIA group (n = 55).

Comparison of pain relief between patient-controlled epidural analgesia and patient-controlled intravenous analgesia for patients undergoing spinal fusion surgeries.

Introduction: This meta-analysis aimed to compare the postoperative analgesic effects of patient-controlled epidural analgesia (PCEA) and patient-controlled intravenous analgesia (PCIA) for patients undergoing spinal fusion surgeries.

Method: Relevant articles were identified using computerized and manual search strategies. Statistical analyses were undertaken by the CMA 2.

Correlations of ezrin expression with pathological characteristics and prognosis of osteosarcoma: a meta-analysis.

We conducted a meta-analysis to comprehensively evaluate the correlations of ezrin expression with pathological characteristics and the prognosis of osteosarcoma. The MEDLINE (1966-2013), the Cochrane Library Database, EMBASE, CINAHL, Web of Science (1945-2013), and the Chinese Biomedical Database were searched without language restrictions. Meta-analyses conducted using STATA software were calculated.