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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.

Tijdschriftbijdrage - Tijdschriftartikel

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 physicochemical
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.
Tijdschrift: European Journal of Medicinal Chemistry
ISSN: 0223-5234
Volume: 166
Pagina's: 1-10
Aantal pagina's: 10
Jaar van publicatie:2019
Trefwoorden:Cancer, Cytotoxic, Hit-to-lead, Leadlikeness, Xanthone, Organische en medische scheikunde