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

Ramdas Vidya, Mari Jean Eggen, Gunda I. Georg, Richard H. Himes

Research output: Contribution to journalArticlepeer-review

16 Scopus citations

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 β isomer (IC50=7.4 μM) is twice as active as cryptophycin-24 (IC50=15 μM).

Original languageEnglish (US)
Pages (from-to)757-760
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume13
Issue number4
DOIs
StatePublished - Feb 2003

Bibliographical note

Funding Information:
We thank the National Institutes of Health (NCI) for financial support (CA 70369). The Department of the Army is acknowledged for post-doctoral fellowships from the Breast Cancer Research Program to M. E. and R. V. This work was supported in part by the Kansas Technology Enterprise Corporation through the Centers of Excellence Program.

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