1. Synthesis and biological activity of polyalthenol and pentacyclindole analogues
- Author
-
Marcos, I. S., Basabe, Pilar, Mollinedo, Faustino, Padrón, José M., Instituto de Salud Carlos III, Red Temática de Investigación Cooperativa en Cáncer (España), European Commission, and Junta de Castilla y León
- Subjects
Pentacyclindole ,Ent-halimic acid ,Antitumourals ,Polyalthenol ,Indole sesquiterpenes - Abstract
A series of indole sesquiterpenes analogues of polyalthenol and pentacyclindole have been synthesized starting from ent-halimic acid in order to test their biological activity. These analogues include diverse oxidation levels at the sesquiterpenyl moiety and different functionalization on the indole ring. All synthetic derivatives were tested against a representative panel of Gram positive and Gram negative bacterial strains, and the human solid tumour cell lines A549 (non-small cell lung), HBL-100 (breast), HeLa (cervix), SW1573 (non-small cell lung), T-47D (breast) and WiDr (colon). Overall, the compounds presented activity against the cancer cell lines. The resulting lead, displaying a polyalthenol scaffold, showed GI50 values in the range 1.2–5.7 μM against all cell lines tested. This research was co-financed by the EU Research Potential (FP7-REGPOT-2012-CT2012-31637-IMBRAIN), the European Regional Development Fund (FEDER), the Spanish Red Temática de Investigación Cooperativa en Cáncer (RD06/0020/1037), the Spanish Instituto de Salud Carlos III (PI11/00840), and the Spanish Junta de Castilla y León (GR-178, SA063A07, GR-15, CSI052A11-2). I.C. acknowledges Junta de Castilla y León for a doctoral fellowship.
- Published
- 2014