Total Synthesis and Anti-Tubulin Activity of Epi-C3 Analogues of Cryptophycin-24
Journal of Medicinal Chemistry2004Vol. 47(14), pp. 3697–3699
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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.
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