We developed a highly potent anticancer
agent, dolastatinol, which
is a methylene hydroxyl derivative of dolastatin 10. Dolastatinol
is a synthetic analog of dolastatin 10, synthesized by a solid-phase
peptide Fmoc chemistry protocol on 2-chlorotrityl chloride resin utilizing
a pH-triggering self-immolative monosuccinate linker. The introduction
of the C-terminus hydroxyl methylene functionality preserves the anticancer
properties of the parent dolastatin 10, including strong suppression
of the cell proliferation, migration, high cytotoxicity. Our research
establishes a new facile route toward the further development of C-terminus-modified
dolastatin-10-based microtubule inhibitors for anticancer treatment.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.