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Updated: Jun 19, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Solid-phase synthesis and biological activity of malformin C and its derivatives
Yasuhiro Kojima1, Toshiaki Sunazuka, Kenichiro Nagai
1Kitasato Institute, Kitasato Institute for Life Science and Graduate School of Infection Control Sciences, Kitasato University, Tokyo, Japan.
Abstract:
We accomplished the solid-phase total synthesis of malformin C, which is adaptable for the easy preparation of various derivatives. A solid-phase total synthesis of malformin C was achieved by on-resin macrolactamization and disulfide bond formation, with concurrent cleavage from the resin. Antimalarial and antitrypanosomal activities were examined, which helped elucidate partial structure-activity relationships. Results indicate that the disulfide bond is essential and branched amino acids are also crucial components if the compound is to exhibit potent antimalarial and antitrypanosomal properties.
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