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Issue 5, 2016
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Identification of noreremophilane-based inhibitors of angiogenesis using zebrafish assays

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Abstract

Noreremophilanes are a rare class of cis-hydrindanes produced by genus Ligularia herbaceous plants which are known to exhibit interesting biological activities. We synthesized cis-hydrindanes based on a naturally occurring noreremophilane scaffold using a Diels–Alder/aldol sequence and screened them for multiple biological activities using high-content zebrafish embryonic development assays. We discovered a noreremophilane that has strong anti-angiogenic effects on the developing zebrafish embryos as well as on tumor-induced angiogenesis in a zebrafish xenograft model. We synthesized several derivatives of this class of noreremophilanes and performed structure–activity relationship studies in zebrafish to identify more potent and less toxic analogs of the original structure.

Graphical abstract: Identification of noreremophilane-based inhibitors of angiogenesis using zebrafish assays

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Publication details

The article was received on 31 Jul 2015, accepted on 08 Oct 2015 and first published on 08 Oct 2015


Article type: Paper
DOI: 10.1039/C5OB01594D
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Citation: Org. Biomol. Chem., 2016,14, 1569-1578

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    Identification of noreremophilane-based inhibitors of angiogenesis using zebrafish assays

    K. M. Muthukumarasamy, K. L. Handore, D. N. Kakade, M. V. Shinde, S. Ranjan, N. Kumar, S. Sehrawat, C. Sachidanandan and D. S. Reddy, Org. Biomol. Chem., 2016, 14, 1569
    DOI: 10.1039/C5OB01594D

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