2. Academic Validation
  3. (+/-)-3,4-Dihydroxy-8,9-methylenedioxypterocarpan and derivatives: cytotoxic effect on human leukemia cell lines

(+/-)-3,4-Dihydroxy-8,9-methylenedioxypterocarpan and derivatives: cytotoxic effect on human leukemia cell lines

  • Eur J Med Chem. 2009 Feb;44(2):920-5. doi: 10.1016/j.ejmech.2008.01.027.
Chaquip D Netto 1,  Eduardo S J Santos,  Carolina Pereira Castro,  Alcides J M da Silva,  Vivian M Rumjanek,  Paulo R R Costa
Affiliations

Affiliation

  • 1 Laboratório de Química Bioorgânica (LQB), Núcleo de Pesquisas de Produtos Naturais, Centro de Ciências da Saúde, Bloco H, Universidade Federal do Rio de Janeiro, RJ 21941-590, Brazil.
PMID: 18468732 DOI: 10.1016/j.ejmech.2008.01.027
Abstract

Naturally occurring pterocarpans 1a,b, pterocarpan 1c, isoflavane 2 and ortho-quinone 3 were synthesized in the racemic form and their cytotoxic effect was evaluated on the human leukemia cell lines K562 (resistant to oxidative stress), Lucena-1 (MDR phenotype) and HL-60. Ortho-quinone 3 (IC(50)=1.5 microM, 1.8 microM and 0.2 microM, respectively) and catechol pterocarpan 1a (IC(50)=3.0 microM, 3.7 microM and 2.1 microM, respectively) were the most active compounds on these cells and were also evaluated on Other human leukemia cell lines (Jurkat and Daudi). Ortho-quinone 3 was 2 to 10 times more potent than pterocarpan 1a, depending on the cell line considered, however, showed a greater toxicity for lymphocytes activated by PHA.

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