Bicyclic radester analogues have been synthesized and evaluated for Hsp90 inhibitory activity. These analogues induce concentration-dependent degradation of Hsp90-dependent client proteins with the six-membered bicyclic analogues manifesting increased activity versus the five-membered counterparts.
Jadhav, V. D., Duerfeldt, A. S., & Blagg, B. S. J. (2009). Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors. Bioorganic & Medicinal Chemistry Letters, 19(24), 6845–6850. http://doi.org/10.1016/j.bmcl.2009.10.091
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