Fungal metabolites: structural diversity as incentive for anticancer drug development

Greve, Hendrik; Mohamed, Ietidal; Pontius, Alexander; Kehraus, Stefan; Gross, Harald; König, Gabriele M.

doi:10.1007/s11101-010-9198-5

Cited by 33 publications

(24 citation statements)

References 64 publications

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“…For example, this diverse data set could be used for HTS to find new hits with new scaffolds and diverse properties. The high and unique scaffold diversity of fungal metabolites revealed in this work, in addition to the high structural complexity and balanced molecular properties revealed in previous studies (Greve et al, 2010; El-Elimat et al, 2012; Cragg and Newman, 2013; Gonzalez-Medina et al, 2016), further supports fungal metabolites as a promising sources of novel compounds for drug discovery.…”

Section: Discussionsupporting

confidence: 79%

Scaffold Diversity of Fungal Metabolites

González-Medina

Owen²,

El‐Elimat

et al. 2017

Front. Pharmacol.

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Many drug discovery projects rely on commercial compounds to discover active leads. However, current commercial libraries, with mostly synthetic compounds, access a small fraction of the possible chemical diversity. Natural products, in contrast, possess a vast structural diversity and have proven to be an outstanding source of new drugs. Several chemoinformatic analyses of natural products have demonstrated their diversity and structural complexity. However, to our knowledge, the scaffold content and structural diversity of fungal secondary metabolites have never been studied. Herein, the scaffold diversity of 223 fungal metabolites was measured and compared to the diversity of approved drugs and commercial libraries for HTS containing natural, synthetic, and semi-synthetic compounds. In addition, the global diversity of the fungal isolates was assessed and compared to other reference data sets using Consensus Diversity Plots, a chemoinformatic tool recently developed. It was concluded that fungal secondary metabolites are cyclic systems with few ramifications and more diverse than the commercial libraries with natural products and semi-synthetic compounds. The fungal metabolites data set was one of the most structurally diverse, containing a large proportion of different and unique scaffolds not found in the other compound data sets including ChEMBL. Therefore, fungal metabolites offer a rich source of molecules suited for identifying diverse candidates for drug discovery.

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Section: Discussionsupporting

confidence: 79%

Scaffold Diversity of Fungal Metabolites

González-Medina

Owen²,

El‐Elimat

et al. 2017

Front. Pharmacol.

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“…The medical applications of sesquiterpenoids as a source of anticancer drugs have been of great interest to the fields of natural products, medicinal chemistry and pharmacology (Adio 2009;Clarke et al, 2006;Chen et al, 2011;Greve et al, 2010;Mahmoud et al, 1980;McMorris 1999). The study enhances appreciation of the potential for the application of sesquiterpenoids with guaiane skeleton, particularly in the inhibition of HL-60, SMMC-7721 and HeLa cell lines.…”

Section: Resultsmentioning

confidence: 98%

Cytotoxic sesquiterpenoids from Senecio densiserratus

Yang

Chen

Wei

et al. 2016

Phytochemistry Letters

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“…Recent years' studies proved that marine fungi are promising sources of new structural and biologically active secondary metabolites (Bhadury et al, 2006;Debbab et al, 2010;Greve et al, 2010;Proksch et al, 2010;Rateb & Ebel, 2011).…”

Section: Marine Fungimentioning

confidence: 99%