Synthesis of thiazolyl-based hydroxamic acids as histone deacetylase inhibitors
نویسندگان
چکیده
منابع مشابه
5-aryl-1,3,4-thiadiazole-based hydroxamic acids as histone deacetylase inhibitors and antitumor agents: synthesis, bioevaluation and docking study.
The search for newer histone deacetylase (HDAC) inhibitors has attracted a great deal of interest of medicinal chemists worldwide, especially after the first HDAC inhibitor (Zolinza(®), widely known as SAHA or Suberoylanilide hydroxamic acid) was approved by the FDA for the treatment of Tcell lymphoma in 2006. As a continuity of our ongoing research in this area, we designed and synthesized a s...
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Histone deacetylases are set of enzymes that have been of interest in drug discovery for the last more than 3 decades. They are responsible for cleaving of acetyl groups from acetyl-lysine residues in histones and various non-histone proteins. Histone deacetylase inhibition is a contemporary, clinically validated therapeutic tactic for cancer treatment. Hydroxamic acid derivatives are among the...
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New thienopyrimidine hydroxamic acid derivatives as HDACs inhibitors were designed, synthesized and evaluated. All compounds were evaluated for their ability to inhibit recombinant human HDAC1, HDAC3, and HDAC6 isoforms and in vitro anti-proliferative activity on tumor cell lines RMPI 8226 and HCT 116. Most of these compounds displayed good to excellent inhibitory activities against HDACs. The ...
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A series of 4-anilinothieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as novel HDACs inhibitors were designed, synthesized and evaluated. Most of these compounds displayed good to excellent inhibitory activities against HDAC1, 3, 6. The IC50 values of compound 10r against HDAC1, HDAC3, HDAC6 was 1.14 ± 0.03 nM, 3.56 ± 0.08 nM, 11.43 ± 0.12 nM. Compound 10r noticeably up-regulated the l...
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A. Al-Hamashi, J. Almaliti, R. Farrell, V. L. Tillekeratne University of Toledo Purpose Histone deacetylase (HDAC) enzymes, which are overexpressed in many cancer tissues, present a potential target for cancer chemotherapy.HDAC inhibitors (HDACis) are currently being investigated as potential anticancer agents. Most of the current HDACis are not selective and have high potential toxicity. Selec...
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ژورنال
عنوان ژورنال: Arkivoc
سال: 2020
ISSN: 1551-7012
DOI: 10.24820/ark.5550190.p011.279