Design, Synthesis, and Structure-Activity relationships of Evodiamine-Based topoisomerase (Top)/Histone deacetylase (HDAC) dual inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2022.105702
Abstract: On the basis of synergistic effect between topoisomerase (Top) and histone deacetylase (HDAC) inhibitors, a series of novel evodiamine-based Top/HDAC dual inhibitors were designed and synthesized. Systematic structure-activity relationship (SAR) studies led to the discovery… read more here.
Keywords: topoisomerase top; evodiamine based; hdac dual; dual inhibitors ... See more keywords
Discovery of novel tubulin/HDAC dual-targeting inhibitors with strong antitumor and antiangiogenic potency.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113790
Abstract: A novel series of cis-diphenylethene and benzophenone derivatives as tubulin/HDAC dual-targeting inhibitors were designed and synthesized. Among them, compound 28g exhibited the most potent antiproliferative activities against six different human cancer cell lines, 28g could… read more here.
Keywords: targeting inhibitors; tubulin hdac; dual targeting; antitumor antiangiogenic ... See more keywords
Rational design and characterization of a DNA/HDAC dual-targeting inhibitor containing nitrogen mustard and 2-aminobenzamide moieties.
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DOI: 10.1039/c7md00476a
Abstract: Histone deacetylases (HDACs) play a key role not only in gene expression but also in DNA repair. Herein, we report the rational design and characterization of a compound named chlordinaline containing nitrogen mustard and 2-aminobenzamide… read more here.
Keywords: mustard aminobenzamide; dual targeting; dna hdac; nitrogen mustard ... See more keywords
Discovery of BRAF/HDAC Dual Inhibitors Suppressing Proliferation of Human Colorectal Cancer Cells
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DOI: 10.3389/fchem.2022.910353
Abstract: The combination of histone deacetylase inhibitor and BRAF inhibitor (BRAFi) has been shown to enhance the antineoplastic effect and reduce the progress of BRAFi resistance. In this study, a series of (thiazol-5-yl)pyrimidin-2-yl)amino)-N-hydroxyalkanamide derivatives were designed… read more here.
Keywords: braf hdac; hdac dual; dual inhibitors; proliferation ... See more keywords