Synthesis, biochemical, pharmacological characterization and in silico profile modelling of highly potent opioid orvinol and thevinol derivatives.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112145
Abstract: Morphine and its derivatives play inevitably important role in the μ-opioid receptor (MOR) targeted antinociception. A structure-activity relationship study is presented for novel and known orvinol and thevinol derivatives with varying 3-O, 6-O, 17-N and… read more here.
Keywords: orvinol thevinol; synthesis biochemical; thevinol derivatives; biochemical pharmacological ... See more keywords
Design, Synthesis, and Biochemical and Biological Evaluation of Novel 7-Deazapurine Cyclic Dinucleotide Analogues as STING Receptor Agonists
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DOI: 10.1021/acs.jmedchem.2c01305
Abstract: Cyclic dinucleotides (CDNs) are second messengers that activate stimulator of interferon genes (STING). The cGAS-STING pathway plays a promising role in cancer immunotherapy. Here, we describe the synthesis of CDNs containing 7-substituted 7-deazapurine moiety. We… read more here.
Keywords: cdns; design synthesis; dinucleotide; synthesis biochemical ... See more keywords
Synthesis and Biochemical Evaluation of Baicalein Prodrugs
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DOI: 10.3390/pharmaceutics13091516
Abstract: Baicalein (5,6,7-trihydroxy-2-phenyl-4H-1-benzopyran-4-one), a flavonoid analog from Scutellaria baicalensis, possesses several pharmacological activities including antioxidant, antiproliferative, and anti-inflammatory activities. We previously reported that baicalein inhibits the thymic stromal lymphopoietin (TSLP)/TSLP receptor (TSLPR) signaling pathways and can… read more here.
Keywords: baicalein; baicalein prodrugs; synthesis biochemical; evaluation baicalein ... See more keywords