2. Academic Validation
  3. Efficiently functionalized oxacalix[4]arenes: Synthesis, characterization and exploration of their biological profile as novel HDAC inhibitors

Efficiently functionalized oxacalix[4]arenes: Synthesis, characterization and exploration of their biological profile as novel HDAC inhibitors

  • Bioorg Med Chem Lett. 2016 Feb 1;26(3):1005-1010. doi: 10.1016/j.bmcl.2015.12.044.
Viren Mehta 1,  Mohd Athar 2,  P C Jha 2,  Manthan Panchal 1,  Krunal Modi 1,  V K Jain 1
Affiliations

Affiliations

  • 1 Gujarat University, Navrangpura, Ahmedabad 380009, India.
  • 2 CCG@CUG Group, School of Chemical Sciences, Central University of Gujarat, Sector-30, Gandhinagar 382030, India.
PMID: 26725026 DOI: 10.1016/j.bmcl.2015.12.044
Abstract

A series of novel substituted oxacalix[4]arene has been synthesized and explored for their biological profile by evaluating Anticancer, Antifungal and Antibacterial properties. The derivatives have been characterized by various spectroscopic techniques such as IR, (1)H NMR, (13)C NMR and Mass spectrometry. Many compounds showed strong inhibition (MIC) in the range of ∼0-50 μM with interesting cytotoxic activities against Hela cells in particular. The compounds were theoretically evaluated by docking studies as potential histone deacetylase inhibitors (HDACi). The study indicates that compounds bound adequately with HDAC, and hence complemented the experimental findings.

Keywords

Anti-cancer activity; Docking; Molecular recognition; Oxacalix[4]arene.

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