Total synthesis and anti-tubulin activity of epi-C3 analogues of cryptophycin-24

Suzanne B. Buck, Jacquelyn K. Huff, Richard H. Himes, Gunda I. Georg

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

Epi-C3-cryptophycin-24, epi-C3-m-chlorobenzyl-cryptophycin-24, and the corresponding styrenes were synthesized and tested in vitro against the MCF-7 and multidrug-resistant MCF-7/ADR breast cancer cell lines and in an in vitro tubulin assembly assay. The results demonstrate that the S configuration at the C3 stereocenter is not required to induce potent cytotoxicity and the m-Cl substituent present on the C10 side chain did not induce any large change in activity.

Original languageEnglish (US)
Pages (from-to)3697-3699
Number of pages3
JournalJournal of medicinal chemistry
Volume47
Issue number14
DOIs
StatePublished - Jul 1 2004

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