Synthesis and antimalarial activity of calothrixins A and B, and their N-alkyl derivatives

Kohji Matsumoto, Tominari Choshi, Mai Hourai, Yoshito Zamami, Kenji Sasaki, Takumi Abe, Minoru Ishikura, Noriyuki Hatae, Tatsunori Iwamura, Shigeo Tohyama, Junko Nobuhiro, Satoshi Hibino

Research output: Contribution to journalArticlepeer-review

55 Citations (Scopus)


We synthesized calothrixin B using our developed biomimetic method and derived N-alkyl-calothrixins A and B. The in vitro antimalarial activity of the calothrixin derivatives, including calothrixins A and B, against the Plasmodium falciparum FCR-3 strain was evaluated. All test compounds exhibited antimalarial activity over a concentration range of 6.4 × 10-6-1.2 × 10-7 M.

Original languageEnglish
Pages (from-to)4762-4764
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Issue number14
Publication statusPublished - Jul 15 2012


  • Antimalarial activity
  • Calothrixin A
  • Calothrixin B
  • Indolo[3,2-j] phenanthridine
  • N-Alkyl-calothrixins

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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