2. Academic Validation
  3. Synthesis and cytotoxic activity evaluation of dihydrocucurbitacin B and cucurbitacin B derivatives

Synthesis and cytotoxic activity evaluation of dihydrocucurbitacin B and cucurbitacin B derivatives

  • Bioorg Med Chem. 2012 May 1;20(9):3016-30. doi: 10.1016/j.bmc.2012.03.001.
Karen Luise Lang 1,  Izabella Thaís Silva,  Lara Almida Zimmermann,  Vanessa Rocha Machado,  Marina Rodrigues Teixeira,  María Ivana Lapuh,  Mariana Alejandra Galetti,  Jorge Alejandro Palermo,  Gabriela Myriam Cabrera,  Lílian Sibelle Campos Bernardes,  Cláudia Maria Oliveira Simões,  Eloir Paulo Schenkel,  Miguel Soriano Balparda Caro,  Fernando Javier Durán
Affiliations

Affiliation

  • 1 Programa de Pós-Graduação em Química, Universidade Federal de Santa Catarina, Florianópolis, SC, Brazil. karenluise@gmail.com
PMID: 22472043 DOI: 10.1016/j.bmc.2012.03.001
Abstract

Two cucurbitacins, dihydrocucurbitacin B (1) and cucurbitacin B (2), which can be obtained in large amounts from the roots of Wilbrandia ebracteata and from the fruits of Luffa operculata, respectively, were used as starting Materials for the preparation of a library of 29 semi-synthetic derivatives. The structural changes that were performed include the removal, modification or permutation of functional groups in rings A and B as well as in the side chain. All new semisynthetic compounds, as well as 1 and 2, were tested in vitro for their cytotoxic effects on non-small-cell lung Cancer cells (A549 cells). Some of these compound displayed potent to moderate activity against A549 tumor cells, especially those cucurbitacin B derivatives which were modified at ring A.

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