Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors

Bhaskar Reddy Kusuma, Adam S. Duerfeldt, Brian S.J. Blagg

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

Novobiocin analogs lacking labile glycosidic ether have been designed, synthesized and evaluated for Hsp90 inhibitory activity. Replacement of the synthetically complex noviose sugar with simple aromatic side chains produced analogs that maintain moderate cytotoxic activity against MCF7 and SkBR3 breast cancer cell-lines. Rationale for the preparation of des-noviose novobiocin analogs in addition to their synthesis and biological evaluation are presented herein.

Original languageEnglish (US)
Pages (from-to)7170-7174
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number23
DOIs
StatePublished - Dec 1 2011
Externally publishedYes

Bibliographical note

Funding Information:
The authors gratefully acknowledge the support of this project by NIH CA120458, the Madison and Lila Self Graduate Fellowship (A.S.D.), the American Foundation of Pharmaceutical Education Pre-doctoral Fellowship (A.S.D.) and the Institute for Advancing Medical Innovation Pre-doctoral Fellowship (A.S.D.) for financial support.

Keywords

  • Chaperone
  • Hsp90
  • Inhibitors
  • Novobiocin

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