Publications
Detailed Information
Design, synthesis and biological evaluation of novel hydroxamic acids bearing artemisinin skeleton
Cited 20 time in
Web of Science
Cited 22 time in Scopus
- Authors
- Issue Date
- 2016-06
- Publisher
- Academic Press
- Citation
- Bioorganic Chemistry, Vol.66, pp.63-71
- Abstract
- A series of novel hydroxamic acids bearing artemisinin skeleton was designed and synthesized. Some compounds in this series exhibited moderate inhibition against the whole cell HDAC enzymes. Especially, compound 6g displayed potent cytotoxicity against three human cancer cell lines, including HepG2 (liver cancer), MCF-7 ( breast cancer) and HL-60 (leukemia cancer), with IC50 values of 2.50, 2.62 and 1.28 mu g/mL, respectively. Docking studies performed with two potent compounds 6a and 6g using Autodock Vina showed that both compounds bound to HDAC2 with relatively high binding affinities from -7.1 to 7.0 kcal/mol compared to SAHA (-7.4 kcal/mol). It was found in this research that most of the target compounds seemed to be more cytotoxic toward blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells. (C) 2016 Elsevier Inc. All rights reserved.
- ISSN
- 0045-2068
- Files in This Item:
- There are no files associated with this item.
- Appears in Collections:
Item View & Download Count
Items in S-Space are protected by copyright, with all rights reserved, unless otherwise indicated.