Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors |
| |
Authors: | Kusuma Bhaskar Reddy Duerfeldt Adam S Blagg Brian S J |
| |
Affiliation: | Department of Medicinal Chemistry, The University of Kansas, Lawrence, KS 66045-7563, USA. |
| |
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. |
| |
Keywords: | Hsp90 Novobiocin Chaperone Inhibitors |
本文献已被 ScienceDirect PubMed 等数据库收录! |