Synthesis of natural phaeosphaeride A derivatives and an in vitro evaluation of their anti-cancer potential.
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.
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: vvaavv@mail.ru.
Victoria V
VV
Abzianidze
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.
Daria S
DS
Prokofieva
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.
Leonid A
LA
Chisty
All-Russian Institute of Plant Protection, Federal Agency of Scientific Organizations, Pushkin, Saint Petersburg 196608, Russian Federation.
Ksenia P
KP
Bolshakova
All-Russian Institute of Plant Protection, Federal Agency of Scientific Organizations, Pushkin, Saint Petersburg 196608, Russian Federation.
Alexander O
AO
Berestetskiy
Department of Crystallography, Institute of Earth Sciences, Saint Petersburg State University, University Emb., 7/9., Saint Petersburg 199034, Russian Federation.
Taras L
TL
Panikorovskii
Department of Organic Chemistry, Institute of Chemistry, Saint Petersburg State University, Universitetsky Pr., 26, Saint Petersburg 198504, Russian Federation.
Alexander S
AS
Bogachenkov
Department of Chemistry and Biochemistry, Old Dominion University, 4541 Hampton Boulevard, Norfolk, VA 23529, United States. Electronic address: aholder@odu.edu.
Alvin A
AA
Holder
D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D018360:Crystallography, X-Ray; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure
D019086:Bridged Bicyclo Compounds, Heterocyclic; C520910:phaeosphaeride A
A549 cancer cell line; Anti-cancer agents; In vitro studies; Natural products; Phaeosphaeride A; X-ray crystallography