Synthesis and evaluation of 8,9-amido analogs of geldanamycin |
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| Authors: | Merritt B Andrus Yong Wong Kristin Beebe |
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| Institution: | a Department of Chemistry and Biochemistry, Brigham Young University, C100 BNSN, Provo, UT 84602, USA
b National Cancer Institute, Building 10-Hatfield CRC, Room 1-5952, 10 Center Drive, Rockville, MD 20892, USA |
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| 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. |
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| Keywords: | Glycolate aldol Ansamycin Geldanamycin Amide isostere Heat-shock protein |
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