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Enhancement of Antiproliferative Activity by Molecular Simplification of Catalpol

AuthorsGarcía, 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.
KeywordsAntitumor agents
Cell cycle
Molecular simplification
Structure elucidation
Issue Date1-Apr-2010
CitationBioorganic and Medicinal Chemistry 18(7): 2515-2523 (2010)
AbstractTwo 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.
Publisher version (URL)https://doi.org/10.1016/j.bmc.2010.02.044
Appears in Collections:(IBMCC) Artículos
(IPNA) Artículos
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