The identification of three distinct but structurally related classes of microbial-derived spliceosome modulators has provided an exciting opportunity for the development of mechanistically new cancer treatments. A team at UC San Diego has undertaken a SAR study on the spliceosome modulator FD-895 that focused on improving compound stability, while retaining potent antiproliferative and splicing activity. This led to the identification of a more potent and stable analog, (17S)-FD-895 (1), and a less active but extremely stable cyclopropane analog 2, which is currently undergoing preclinical evaluation. These analogs will serve as templates for next generation spliceosome modulating anticancer drugs. © 2013 American Chemical Society.
CITATION STYLE
Butler, M. S. (2013, September 12). Remediating cancer via splicing modulation. Journal of Medicinal Chemistry. https://doi.org/10.1021/jm401289z
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