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  3. All that glitters is not gold: Panning cytotoxic natural products and derivatives with a fused tricyclic backbone by the estimation of their leadlikeness for cancer treatment

All that glitters is not gold: Panning cytotoxic natural products and derivatives with a fused tricyclic backbone by the estimation of their leadlikeness for cancer treatment

  • Eur J Med Chem. 2019 Mar 15:166:1-10. doi: 10.1016/j.ejmech.2019.01.028.
Luiz Carlos Klein-Júnior 1,  Rogério Corrêa 2,  Yvan Vander Heyden 3,  Valdir Cechinel Filho 2
Affiliations

Affiliations

  • 1 Chemical-Pharmaceutical Investigation Center, University do Vale do Itajaí - UNIVALI, Rua Uruguai 456, 88.302-202, Itajaí, SC, Brazil. Electronic address: lcklein@univali.br.
  • 2 Chemical-Pharmaceutical Investigation Center, University do Vale do Itajaí - UNIVALI, Rua Uruguai 456, 88.302-202, Itajaí, SC, Brazil.
  • 3 Department of Analytical Chemistry, Applied Chemometrics and Molecular Modelling, Center for Pharmaceutical Research (CePhaR), Vrije Universiteit Brussel - VUB, Laarbeeklaan 103, 1090, Brussels, Belgium.
PMID: 30684866 DOI: 10.1016/j.ejmech.2019.01.028
Abstract

Tricyclic compounds call the attention because of their pharmacological properties, and are considered a preferred platform for the development of drugs. Especially, in Cancer treatment, these planar compounds are known for their ability to stack with DNA base pairs, acting as intercalators. In this sense, Natural Products (NPs) are a prodigal source of polycyclic compounds, comprising classes, such as carbolines, Anthraquinones and Xanthones. However, most of these compounds lack suitable physico-chemical properties, compatible to oral bioaviability. In this perspective, this paper aims to overview the role of tricyclic cores in the development of cytotoxic compounds, focusing on the leadlikeness estimation of the most prominent NP classes and their synthetic derivatives.

Keywords

Cancer; Cytotoxic; Hit-to-lead; Leadlikeness; Xanthone.

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