Halogenation at the Phenylalanine Residue of Monomethyl Auristatin F Leads to a Favorable <i>cis</i>/<i>trans</i> Equilibrium and Retained Cytotoxicity.

The auristatin core is sensitive toward modifications, and often tinkering with the molecular structure leads to a significant reduction or complete loss of cytotoxicity. Until now, no practical attempt focused on shifting the cis / trans equilibrium has been reported, with the exception of our recent computational study on the rational design of improved auristatins, 27 which suggested that there might be significant potential embedded in such an approach.

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