Design and Synthesis of C3‐Substituted β‐Carboline‐Based Histone Deacetylase Inhibitors with Potent Antitumor Activities
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DOI: 10.1002/cmdc.201700133
Abstract: A series of hydroxamic acid histone deacetylase (HDAC) inhibitors in which the β‐carboline motif has been incorporated were designed and synthesized. The effect of substitution at the C3 amide on HDAC inhibition and antiproliferative activities… read more here.
Keywords: design synthesis; histone; carboline based; histone deacetylase ... See more keywords
Exploration of TRPM8 Binding Sites by β-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.0c00816
Abstract: Transient receptor potential melastatin 8 (TRPM8) ion channel represents a valuable pharmacological option for several therapeutic areas. Here, a series of conformationally restricted derivatives of the previously described TRPM8 antagonist N,N′-dibenzyl tryptophan 4 were prepared… read more here.
Keywords: vivo; trpm8 binding; binding sites; sites carboline ... See more keywords