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
  • 1. Instituto Universitario de Bio-Orgánica 'Antonio González' (IUBO-AG), Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain. [email protected]
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.