Synthesis of natural phaeosphaeride A derivatives and an in vitro evaluation of their anti-cancer potential.

Abstract

Derivatives of phaeosphaeride A (PPA) were synthesised and characterised; then anti-cancer studies were carried out on the A549 cancer cell line. It was found that the acetyl derivative (compound 3) displayed comparable in vitro cytotoxicity to that of PPA (EC50=49±7 μM and EC50=46±5 μM, respectively), while chloroacetyl derivative 6 (EC50=33±7 μM) was found to have better efficacy towards the A549 cancer cell line.

• Authors: Victoria V Abzianidze, Daria S Prokofieva, Leonid A Chisty, Ksenia P Bolshakova, Alexander O Berestetskiy, Taras L Panikorovskii, Alexander S Bogachenkov, Alvin A Holder
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 25 Issue 23 Pg. 5566-9 (Dec 01 2015) ISSN: 1464-3405 [Electronic] England
• PMID: 26508550 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2015 Elsevier Ltd. All rights reserved.

Chemical References

• Bridged Bicyclo Compounds, Heterocyclic
• phaeosphaeride A

Topics

• Bridged Bicyclo Compounds, Heterocyclic (chemical synthesis, chemistry, pharmacology)
• Cell Line, Tumor
• Cell Survival (drug effects)
• Crystallography, X-Ray
• Drug Screening Assays, Antitumor
• Humans
• Molecular Structure