Actin-binding marine macrolides, such as mycalolides A–C, are potent cytotoxins with nanomolar IC50 values against a range of cancer cell lines. Using a combination of molecular modeling and X-ray data we have identified key pharmacophores that are responsible for actin-binding and designed several truncated mycalolide analogs. This seminar describes the synthesis of a series of analogs which are half the molecular weight of the mycalolides and show promising in vitro inhibition of actin polymerization and tumor cell invasion.

Truncated analogs of actin-targeting natural products: Synthesis and in vitro activity

254th National Meeting (2017)

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