Enhancement of Antiproliferative Activity by Molecular Simplification of Catalpol

Two iridoid scaffolds were synthesized enantioselectively using as key step an l-proline-catalyzed α-formyl oxidation. The in vitro antiproliferative activities were evaluated against a representative panel of human solid tumor cell lines. Both iridoids induced considerably growth inhibition in the range 0.38–1.86 μM. Cell cycle studies for these compounds showed the induction of cell cycle arrest at the G1 phase. This result was consistent with a decrease in the expression of cyclin D1. Damaged cells underwent apoptosis as indicated by specific Annexin V staining.

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Bibliographic Details
Main Authors: García, Celina, León, Leticia G, Pungitore, Carlos R., Ríos-Luci, Carla, Hernández Daranas, Antonio, Montero, Juan Carlos, Pandiella, Atanasio, Tonn, Carlos E., Martín, Víctor S., Padrón, José M.
Other Authors: Ministerio de Educación y Ciencia (España)
Format: artículo biblioteca
Language:English
Published: Elsevier 2010-04-01
Subjects:Antitumor agents, Catalpol, Cell cycle, Molecular simplification, Structure elucidation,
Online Access:http://hdl.handle.net/10261/213312
http://dx.doi.org/10.13039/100007650
http://dx.doi.org/10.13039/501100002923
http://dx.doi.org/10.13039/501100003074
http://dx.doi.org/10.13039/501100007757
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