Document Detail

Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death.
MedLine Citation:
PMID:  25176189     Owner:  NLM     Status:  Publisher    
The synthesis and bio-evaluation of naturally occurring boswellic acids (BAs) as an alternate CAP for the design of new HDAC inhibitors is described. All the compounds were screened against a panel of human cancer cell lines to identify leads, which were subsequently examined for their potential to inhibit HDACs. The identified lead compound showed IC50 value of 6μm for HDACs, found to induce G1 cell cycle arrest at significantly low concentration (1μM) and caused significant loss in mitochondrial membrane potential at 5 and 10μM. Furthermore, specific interactions of the lead molecule inside the catalytic domain were also studied through in silico molecular modeling.
Simmi Sharma; Javeed Ahmad Bhat; Mudassier Ahmad; Arvind Kumar; Manjeet Kumar; Mohmmad Afzal Zargar; Abid Hamid; Bhahwal Ali Shah
Related Documents :
12372989 - Increase in mitochondrial mass in human fibroblasts under oxidative stress and during r...
19634139 - Chronic cigarette smoke extract treatment selects for apoptotic dysfunction and mitocho...
14678389 - Investigation of sequential mitomycin c and photodynamic therapy in a mitomycin-resista...
10198289 - Subcellular heterogeneity of mitochondrial membrane potential: relationship with organe...
12428729 - Acute mitochondrial and chronic toxicological effects of 1-methyl-4-phenylpyridinium in...
20562029 - Tip47 protects mitochondrial membrane integrity and inhibits oxidative-stress-induced c...
15063529 - Single neurons as experimental systems in molecular biology.
20462289 - Surface tension and modeling of cellular intercalation during zebrafish gastrulation.
19609709 - Cancers and the concept of cell senescence.
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-8-14
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2014 Aug 
Date Detail:
Created Date:  2014-9-1     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2014 Elsevier Ltd. All rights reserved.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Development of the excimer probe responsible for DNA target bearing the silylated pyrenes at base mo...
Next Document:  The discovery of potent glycine transporter type-2 inhibitors: Design and synthesis of phenoxymethyl...