Solid-phase synthesis of 2 '-hydroxychalcones. Effects on cell growth inhibition, cell cycle and apoptosis of human tumor cell lines

• Type: Article in International Scientific Journal
• Date: 2012

Authors

Marta Perro Neves (Author) Other; Sara Cravo (Author) FFUP; Raquel T Lima (Author) Other; Helena Vasconcelos, MH (Author) FFUP; Sao Jose Nascimento, MSJ (Author) FFUP; Artur M S Silva (Author) Other; Madalena Pinto (Author) FFUP; Honorina Cidade (Author) FFUP; Arlene G Correa (Author) Other

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 20

Pages: 25-33

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 25 Citations

Scopus - 32 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: P-002-HBM

DOI: 10.1016/j.bmc.2011.11.042

Abstract (EN): Thirty-one 2'-hydroxychalcones were prepared via solid-phase synthesis by base-catalyzed aldol condensation of substituted 2'-hydroxyacetophenones and benzaldehydes. Chalcones were tested for their growth inhibitory activity in three human tumor cell lines (MCF-7, NCI-H460 and A375-C5) using the SRB assay. Results revealed that several of the tested compounds caused a pronounced dose-dependent growth inhibitory effect on the tumor cell lines studied in the low micromolar range. To gain further insight on the cellular mechanism of action of this class of compounds, studies of their effect on cell cycle profile as well as on induction of cellular apoptosis were also carried out. Generally, the tested chalcones interfered with the cell cycle profile and increased the percentage of apoptotic MCF-7 cells. The results here presented may help to identify new chalcone-like structures with optimized cell growth inhibitory activity which may be further tested as potential antitumor agents.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9