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Article Name - Design, synthesis, and antiproliferative activity evaluation of novel N-hydroxyurea derivatives as possible dual HDAC-BET inhibitors

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  • Keywords n-hydroxyurea derivatives, zinc-binding group, docking study, hdac inhibitors, bromodomain ... 2024-08-05
  • Introduction Histone Deacetylases (HDACs) are a family of enzymes that responsible for the reversible acetylation of lysine side chains on the surfaces of enzymes and other proteins comprises a vital regulatory st ... 2024-08-05
  • Experimental Materials and method Chemicals and solvents were utilized as obtained from the supplier, and used without additional purification. The 0.2 mm pre-coated TLC-sheets Alugram® Xtra SIL G/UV254 (Mach ... 2024-08-05
  • Results and Discussion Molecular docking To evaluate the in silico potency and selectivity for Va and Vb, a molecular docking study was carried out on variant HDAC isoforms of HDAC2, HDAC6, HDAC8, in addition to BRD4. Th ... 2024-08-05
  • Conclusion New HDAC/BET inhibitors were designed by the instillation of new zinc binding group of N-hydroxyurea. The molecular docking studies showed an acceptable virtual interaction with both HDAC and BET enzy ... 2024-08-05
  • Funding The work is partially funded by the College of Pharmacy, University of Baghdad ... 2024-08-05
  • Authors Contribution Authors are equally contributed ... 2024-08-05
  • Conflict of Interests Author declared that there is no conflict of interest. ... 2024-08-05
  • References Porter NJ, Christianson DW. Structure, mechanism, and inhibition of the zinc-dependent histone deacetylases. Curr Opin Struct Biol. 2019;59:9–18. [Google Scholar] [CrossRef] ... 2024-08-05