Biologically active quinazoline-based hydroxamic acids
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DOI: 10.1007/s00044-020-02530-7
Abstract: Molecular hybridization has become a new promising way to treat multifactorial diseases with a single compound that acts on multiple targets. The combination of several functional pharmacophore groups in one molecule can lead to a… read more here.
Keywords: based hydroxamic; quinazoline based; active quinazoline; chemistry ... See more keywords
Exploration of certain 1,3-oxazole- and 1,3-thiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103988
Abstract: Several novel series of hydroxamic acids bearing 2-benzamidooxazole/thiazole (5a-g, 6a-g) or 2-phenylsulfonamidothiazole (8a-c) were designed and synthesized. The compounds were obtained straightforwards via a two step pathway, starting from commercially available ethyl 2-aminooxazole-4-carboxylate or ethyl… read more here.
Keywords: based hydroxamic; inhibitors antitumor; hydroxamic acids; thiazole based ... See more keywords
Design, synthesis, and biological evaluation of indole-based hydroxamic acid derivatives as histone deacetylase inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113893
Abstract: The equilibrium between histone acetylation and deacetylation plays an important role in cancer initiation and progression. The histone deacetylases (HDACs) are a class of key regulators of gene expression that enzymatically remove an acetyl moiety… read more here.
Keywords: based hydroxamic; design synthesis; hydroxamic acid; acid derivatives ... See more keywords
Quinazolin-2,4-dione-Based Hydroxamic Acids as Selective Histone Deacetylase-6 Inhibitors for Treatment of Non-Small Cell Lung Cancer.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01590
Abstract: We designed and synthesized quinazolin-2,4-dione-based hydroxamic acids to serve as selective competitive inhibitors of histone deacetylase-6 (HDAC6). The most potent and selective compound, 3d (IC50, 4 nM, HDAC6; IC50 > 10 μM, HDAC1), substantially increased… read more here.
Keywords: based hydroxamic; quinazolin dione; lung cancer; cancer ... See more keywords
Synthesis and HDAC inhibitory activity of pyrimidine-based hydroxamic acids
Sign Up to like & getrecommendations! Published in 2022 at "Beilstein Journal of Organic Chemistry"
DOI: 10.3762/bjoc.18.84
Abstract: Histone deacetylases (HDACs) play an essential role in the transcriptional regulation of cells through the deacetylation of nuclear histone and non-histone proteins and are promising therapeutic targets for the treatment of various diseases. Here, the… read more here.
Keywords: based hydroxamic; synthesis hdac; group; pyrimidine based ... See more keywords