Isolation and Total Synthesis of Kinenzoline, an Antitrypanosomal Linear Depsipeptide Isolated from a Marine Salileptolyngbya sp. Cyanobacterium

Naoaki Kurisawa, Keisuke Otomo, Arihiro Iwasaki, Ghulam Jeelani, Tomoyoshi Nozaki, Kiyotake Suenaga

Research output: Contribution to journalArticlepeer-review

Abstract

Kinenzoline (1), a new linear depsipeptide, was isolated from a marine Salileptolyngbya sp. cyanobacterium. Its structure was elucidated by spectroscopic analyses and degradation reactions. In addition, we achieved a total synthesis of 1 and confirmed its structure. Kinenzoline (1) showed highly selective antiproliferative activity against the causative organism of sleeping sickness, Trypanosoma brucei rhodesiense (IC50 4.5 μM), compared to normal human cells (WI-38, IC50 > 100 μM). Kinenzoline (1) is a promising lead compound for the development of new antitrypanosomal drugs.

Original languageEnglish
Pages (from-to)12528-12536
Number of pages9
JournalJournal of Organic Chemistry
Volume86
Issue number18
DOIs
Publication statusPublished - 2021 Sep 17

ASJC Scopus subject areas

  • Organic Chemistry

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