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Synthesis and evaluation of 8,9-amido analogs of geldanamycin

✍ Scribed by Merritt B. Andrus; Yong Wong; Jing Liu; Kristin Beebe; Leonard M. Neckers

Publisher
Elsevier Science
Year
2009
Tongue
French
Weight
397 KB
Volume
50
Category
Article
ISSN
0040-4039

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✦ Synopsis

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.

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