2. Academic Validation
  3. Synthesis and cytotoxic evaluation of C-9 oxidized podophyllotoxin derivatives

Synthesis and cytotoxic evaluation of C-9 oxidized podophyllotoxin derivatives

  • Bioorg Med Chem. 2007 Feb 15;15(4):1670-8. doi: 10.1016/j.bmc.2006.12.008.
Ma Angeles Castro 1,  José M Miguel del Corral,  Marina Gordaliza,  Pablo A García,  Ma Antonia Gómez-Zurita,  Arturo San Feliciano
Affiliations

Affiliation

  • 1 Departamento de Química Farmacéutica, Facultad de Farmacia, Campus Miguel de Unamuno, Universidad de Salamanca, 37007 Salamanca, Spain. macg@usal.es
PMID: 17197187 DOI: 10.1016/j.bmc.2006.12.008
Abstract

A series of podophyllotoxin and podophyllic aldehyde derivatives, lacking the lactone ring and oxidized at C-9 position, has been prepared. The functionalities considered at C-9 were carboxylic acids and several derivatives such as esters, amides, nitriles or anhydrides. The synthesized compounds were cytotoxic at the micromolar level, though less potent and selective than the parent compounds, revealing the influence of the C-9 electrophilic character on the potency and selectivity of these cyclolignans.

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