Literature DB >> 26725026

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

Viren Mehta1, Mohd Athar2, P C Jha2, Manthan Panchal1, Krunal Modi1, V K Jain1.   

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.
Copyright © 2015 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh:

Substances:

Year:  2015        PMID: 26725026     DOI: 10.1016/j.bmcl.2015.12.044

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Discovery of novel N-substituted thiazolidinediones (TZDs) as HDAC8 inhibitors: in-silico studies, synthesis, and biological evaluation.

Authors:  Neha Upadhyay; Kalpana Tilekar; Niklas Jänsch; Markus Schweipert; Jessica D Hess; Luca Henze Macias; Piotr Mrowka; Renato J Aguilera; Jun-Yong Choe; Franz-Josef Meyer-Almes; C S Ramaa
Journal:  Bioorg Chem       Date:  2020-05-15       Impact factor: 5.275

2.  Analyses of variants of the Ser/Thr dehydratase IlvA provide insight into 2-aminoacrylate metabolism in Salmonella enterica.

Authors:  Andrew J Borchert; Diana M Downs
Journal:  J Biol Chem       Date:  2018-10-16       Impact factor: 5.157

Review 3.  Antimicrobial Activity of Calixarenes and Related Macrocycles.

Authors:  Dmitriy N Shurpik; Pavel L Padnya; Ivan I Stoikov; Peter J Cragg
Journal:  Molecules       Date:  2020-11-05       Impact factor: 4.411

  3 in total

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