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

Bioorganic & Medicinal Chemistry Letters
2003.0

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).

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