Enhancement of antiproliferative activity by molecular simplification of catalpol

Bioorg Med Chem. 2010 Apr 1;18(7):2515-23. doi: 10.1016/j.bmc.2010.02.044.

Celina García ¹, Leticia G León, Carlos R Pungitore, Carla Ríos-Luci, Antonio H Daranas, Juan C Montero, Atanasio Pandiella, Carlos E Tonn, Víctor S Martín, José M Padrón

Affiliations

Affiliation

1 Instituto Universitario de Bio-Orgánica 'Antonio González' (IUBO-AG), Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain. cgargon@ull.es

PMID: 20231098 DOI: 10.1016/j.bmc.2010.02.044

Abstract

Two iridoid scaffolds were synthesized enantioselectively using as key step an l-proline-catalyzed alpha-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 0.38-1.86muM. Cell cycle studies for these compounds showed the induction of cell cycle arrest at the G(1) 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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