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Chromatographic enantiomer separations of different oxazepine indole derivatives were performed using a molecularly imprinted polymer. A 5aR,12R,13S-trans-6,6-dimethyl-12,13-dihydro-6H-5a, 1 3-methanoindolo[2,1-b][1,3]naphthoxazepine-12-carboxamide enantiomerderivative was used as a template and the resultant polymer has shown enantiomer recognition for series of template related compounds. The mechanistic description of the chiral discrimination process is scrutinised, comparing the discrimination between the different conformations and substituents of the oxazepine indoles.
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http://dx.doi.org/10.1002/jssc.200301675 | DOI Listing |
Molecules
July 2023
School of Pharmacy and Bioengineering, Keele University, Newcastle-under-Lyme ST5 5BG, UK.
Phosphatidylcholine-specific phospholipase C (PC-PLC) is an enzyme that catalyzes the formation of the important secondary messengers phosphocholine and diacylglycerol (DAG) from phosphatidylcholine. Although PC-PLC has been linked to the progression of many pathological conditions, including cancer, atherosclerosis, inflammation and neuronal cell death, studies of PC-PLC on the protein level have been somewhat neglected with relatively scarce data. To date, the human gene expressing PC-PLC has not yet been found, and the only protein structure of PC-PLC that has been solved was from (PC-PLC).
View Article and Find Full Text PDFJ Dermatol Sci
September 2020
Hunan Engineering Research Center of Skin Health and Disease, Xiangya Hospital, Central South University, Changsha, China. Electronic address:
Skin diseases bring great psychological and physical impacts on patients, however, a considerable number of skin diseases still lack effective treatments, such as psoriasis, systemic lupus erythematosus, melanoma and so on. Receptor-interacting serine threonine kinase 1 (RIPK1) plays an important role in cell death, especially necroptosis, associated with inflammation and tumor. As many molecules modulate the ubiquitination of RIPK1, disruption of this checkpoint can lead to skin diseases, which can be ameliorated by RIPK1 inhibitors.
View Article and Find Full Text PDFSci Rep
February 2020
Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raibareli Road, Lucknow, 226025, India.
An amendment to this paper has been published and can be accessed via a link at the top of the paper.
View Article and Find Full Text PDFSci Rep
April 2018
Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raibareli Road, Lucknow, 226025, India.
Inspired by the well-documented tumor protecting ability of paullones, recently, we synthesized novel paullone-like scaffolds, indole-fused benzo-oxazepines (IFBOs), and screened them against hepatocellular carcinoma (HCC) specific Hep-G2 cells. Three of the synthesized compounds significantly attenuated the progression of HCC in vitro. By computational studies, we further discovered that IFBOs exhibited a stable binding complex with the IL-6 receptor.
View Article and Find Full Text PDFLife Sci
May 2018
Department of Pharmaceutical Sciences, Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raibareli Road, Lucknow 226025, India. Electronic address:
Aims: To potentiate the well-documented tumor protecting ability of paullones, literatures demand for rational modifications in paullone ring structure and exploration of a precise mechanism underlying their antitumor effects. Thus, recently we synthesized novel paullone-like scaffold, 5H-benzo [2, 3][1,4]oxazepino[5,6-b]indoles, where compounds 13a and 14a attenuated the growth of liver cancer specific Hep-G2 cells in vitro and formed stable binding complex with IL-6. Henceforth, we hypothesized that this action is probably due to the blockade of IL-6 mediated JAK2/STAT3 signaling cascade.
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