| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 5271534 | Tetrahedron Letters | 2009 | 4 Pages |
Abstract
Amido analogs of geldanamycin, an ansamycin anticancer agent, were designed, synthesized, and assayed with SKBR3 cells, in which stability of HER2 receptor tyrosine kinase is dependent on the chaperone Hsp90. An amide was employed as a trisubstituted alkene isostere at the C8,9 position, which provided for a simplified, convergent synthesis through two major fragments, an aniline-amine left-hand portion and a dicarboxylic acid right-hand piece.
Graphical abstractC8,9-Amido isostere analogs of the ansamycin Hsp90 inhibitor geldanamycin were synthesized and evaluated.Download full-size image
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Merritt B. Andrus, Yong Wong, Jing Liu, Kristin Beebe, Leonard M. Neckers,