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Wang Y.-Y.,Key Laboratory of Chemical Biology | Liu J.-Z.,Key Laboratory of Chemical Biology | Yu X.-Y.,Key Laboratory of Chemical Biology | Yang D.-Z.,Key Laboratory of Chemical Biology | And 2 more authors.
Chemical Research in Chinese Universities | Year: 2013

A series of hydrazine and oxadiazole analogs of Sorafenib was designed, synthesized and characterized by proton nuclear magnetic resonance(1H NMR) spectrometry and high resolution mass spectrometry(HRMS). The antiproliferative activities of these compounds against human colorectal carcinoma(HCT-116) and human breast cancer (MDA-MB-231) tumor cell lines were evaluated in vitro by MTT method[MTT=3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide]. The bioassay results suggest that most of the synthesized compounds have antitumor potential to HCT-116 cell line compared with MDA-MB-231 cell line. Compounds 8a, 8b, 8d, 8e, 9f and 9j competitive with Sorafenib demonstrated antiproliferative activities on HCT-116 cell line. © 2013 Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH. Source


Zheng H.,Key Laboratory of Chemical Biology | Li L.,Key Laboratory of Chemical Biology | Sun B.,Key Laboratory of Chemical Biology | Sun B.,Shandong University | And 2 more authors.
Journal of Medicinal Chemistry | Year: 2016

Paraptosis is nonapoptotic cell death characterized by massive endoplasmic reticulum (ER)- or mitochondria-derived vacuoles. Induction of paraptosis offers significant advantages for the treatment of chemotherapy-resistant tumors compared with anticancer drugs that rely on apoptosis. Because some natural alkaloids induce paraptotic cell death, a novel series of benzo[a]quinolizidine derivatives were synthesized, and their antiproliferative activity and ability to induce cytoplasmic vacuolation were analyzed. Structural optimization led to the identification of the potent compound 22b, which inhibited cancer cell proliferation in vitro and in vivo and profoundly facilitated paraptosis-like cell death and induced caspase-dependent apoptosis. Further investigation revealed that 22b-mediated vacuolation originated from persistent ER stress and upregulation of LC3B. Paraptosis induced by benzo[a]quinolizidine derivatives thus represents an alternative strategy for cancer chemotherapy. © 2016 American Chemical Society. Source


Zhao Y.,Hebei University | Zhao Y.,Key Laboratory of Analytical Science and Technology | Zhao Y.,Key Laboratory of Chemical Biology | Liu L.,Hebei University | And 8 more authors.
Chinese Journal of Chromatography (Se Pu) | Year: 2013

An analytical method for the simultaneous determination of 18α-glycyrrhizic acid, 18β-glycyrrhizinic acid, related substances A and B and drug quality standard by reversed-phase high performance liquid chromatography (RP-HPLC) was established. The assay was carried out on a Durashell-Cl8 column (250 mm ×4. 6 mm, 5 μm) with 10 mmol/L ammonium perchlo-rate (the pH value was adjusted to 8.20 with ammonia)-methanol (48: 52, v/v) as mobile phase at a flow rate of 0. 80 mL/min, and the detection wavelength was set at 254 nm. The column temperature was 50 °C and the injection volume was 10 (xL. Under the separation conditions, the calibration curves of the analytes showed good linearities within the mass concentrations of 0. 50 - 100 mg/L (r >0. 999 9). The detection limits for 18α-glycyrrhizic acid, 18β-gly-cyrrhizinic acid, related substances A and B were 0. 15, 0. 10, 0. 10, 0. 15 mg/L, respectively. The average recoveries were between 97. 32% and 99. 33% (n = 3) with the relative standard deviations (RSDs) between 0. 05% and 1. 06%. The method is sensitive, reproducible, and the results are accurate and reliable. The method can be used for the determination of principal components and related substances of ammonium glycyrrhizinate for the quality control of raw material drug of ammonium glycyrrhizinate. Source


Wang X.,Key Laboratory of Chemical Biology | Huang B.,Key Laboratory of Chemical Biology | Suzuki T.,Kyoto Prefectural University of Medicine | Suzuki T.,Japan Science and Technology Agency | And 2 more authors.
Epigenomics | Year: 2015

LSD1 is an epigenetic modulator associated with transcriptional regulation of genes involved in a broad spectrum of key cellular processes, and its activity is often altered under pathological conditions. LSD1 inhibitors are considered to be candidates for therapy of cancer, viral diseases and neurodegeneration. Many LSD1 inhibitors with various scaffolds have been disclosed, and a few potent molecules are in different stages of clinical development. In this review, we summarize recent biological findings on the roles of LSD1 and the current understanding of the clinical significance of LSD1, and focus on the medicinal chemistry strategies used in the design and development of LSD1 inhibitors as drug-like epigenetic modulators since 2012, including a brief consideration of structure-activity relationships. © 2015 Future Medicine Ltd. Source


Xiao R.,Key Laboratory of Chemical Biology | Xiao R.,Shanxi University | Gao Y.,Key Laboratory of Chemical Biology | Gao Y.,Shanxi University | And 7 more authors.
Cell Biology International | Year: 2013

The eukaryotic class II polypeptide chain release factor (eRF3) is an eRF1- and ribosome-dependent GTPase involved in translation termination of protein biosynthesis. eRF3 is a multifunctional protein that is also involved in chromosomal segregation and cytokinesis during mitosis. Survivin is a member of the inhibitor of apoptosis protein (IAP) family that is involved in the organisation of spindle and cell apoptosis. Interaction between survivin and eRF3a-F3 or eRF3b, encoded by the GSPT1 and GSPT2 genes, respectively, was confirmed using yeast two-hybrid (Y2H) and pull-down assays in vitro, and coimmunoprecipitation in vivo. The domains involved in the formation of the survivin-eRF3s complex have been identified. The sites on survivin that interact with eRF3 are located in the baculovirus IAP repeat domain (residues 65-76), which forms a betastrand structure with an overall negative charge. The sites on eRF3 that interact with survivin were localised to the N-terminal domain(NTD; residues 131-200). Cell localisation experiments indicate that both factors are in the nucleus, suggesting that they cooperatively function in nuclear processes. © 2013 International Federation for Cell Biology. Source

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