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ID: ALA1136604

Journal: Bioorg Med Chem Lett

Title: Cryptophycin affinity labels: synthesis and biological activity of a benzophenone analogue of cryptophycin-24.

Authors: Vidya R, Eggen M, Georg GI, Himes RH.

Abstract: An efficient synthesis of a C16 side chain benzophenone analogue of cryptophycin-24 using a crotylboration reaction and Heck coupling as key steps is described. In an in vitro tubulin assembly assay, the benzophenone analogue of the beta isomer (IC(50)=7.4 microM) is twice as active as cryptophycin-24 (IC(50)=15 microM).

CiteXplore: 12639575

DOI: 10.1016/s0960-894x(02)01023-5