2. Academic Validation
  3. Synthesis, cytotoxicity and antiplasmodial activity of novel ent-kaurane derivatives

Synthesis, cytotoxicity and antiplasmodial activity of novel ent-kaurane derivatives

  • Eur J Med Chem. 2013 Apr:62:168-76. doi: 10.1016/j.ejmech.2012.12.010.
Ronan Batista 1,  Pablo A García,  María Angeles Castro,  José M Miguel Del Corral,  Nivaldo L Speziali,  Fernando de P Varotti,  Renata C de Paula,  Luis F García-Fernández,  Andrés Francesch,  Arturo San Feliciano,  Alaíde B de Oliveira
Affiliations

Affiliation

  • 1 Departamento de Estudos Básicos e Instrumentais, Universidade Estadual do Sudoeste da Bahia, BR 415, Km 03, s/n°, 45.700-000 Itapetinga, Bahia, Brazil.
PMID: 23353738 DOI: 10.1016/j.ejmech.2012.12.010
Abstract

This paper reports on the syntheses and spectrometric characterisation of eleven novel ent-kaurane Diterpenoids, including a complete set of (1)H, (13)C NMR and crystallographic data for two novel ent-kaurane diepoxides. Moreover, the antineoplastic cytotoxicity for kaurenoic acid and the majority of ent-kaurane derivatives were assessed in vitro against a panel of fourteen Cancer cell lines, of which allylic alcohols were shown to be the most active compounds. The good in vitro antimalarial activity and the higher selectivity index values observed for some ent-kaurane epoxides against the chloroquine-resistant W2 clone of Plasmodium falciparum indicate that this class of Natural Products may provide new hits for the development of antimalarial drugs.

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