Synthesis of natural phaeosphaeride A derivatives and an in vitro evaluation of their anti-cancer potential
- Bioorg Med Chem Lett. 2015 Dec 1;25(23):5566-9. doi: 10.1016/j.bmcl.2015.10.048.
Affiliations
- 1. Chemical Modeling Laboratory, Research Institute of Hygiene, Occupational Pathology and Human Ecology, Federal Medical Biological Agency, p/o Kuz'molovsky, Saint Petersburg 188663, Russian Federation. Electronic address: [email protected].
- 2. Chemical Modeling Laboratory, Research Institute of Hygiene, Occupational Pathology and Human Ecology, Federal Medical Biological Agency, p/o Kuz'molovsky, Saint Petersburg 188663, Russian Federation.
- 3. All-Russian Institute of Plant Protection, Federal Agency of Scientific Organizations, Pushkin, Saint Petersburg 196608, Russian Federation.
- 4. Department of Crystallography, Institute of Earth Sciences, Saint Petersburg State University, University Emb., 7/9., Saint Petersburg 199034, Russian Federation.
- 5. Department of Organic Chemistry, Institute of Chemistry, Saint Petersburg State University, Universitetsky Pr., 26, Saint Petersburg 198504, Russian Federation.
- 6. Department of Chemistry and Biochemistry, Old Dominion University, 4541 Hampton Boulevard, Norfolk, VA 23529, United States. Electronic address: [email protected].
PMID: 26508550
DOI: 10.1016/j.bmcl.2015.10.048
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.
Keywords
A549 cancer cell line; Anti-cancer agents; In vitro studies; Natural products; Phaeosphaeride A; X-ray crystallography.