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

Authors :
Arihiro Iwasaki
Tomoyoshi Nozaki
Kiyotake Suenaga
Naoaki Kurisawa
Keisuke Otomo
Ghulam Jeelani
Source :
The Journal of Organic Chemistry. 86:12528-12536
Publication Year :
2021
Publisher :
American Chemical Society (ACS), 2021.

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.

Details

ISSN :
15206904 and 00223263
Volume :
86
Database :
OpenAIRE
Journal :
The Journal of Organic Chemistry
Accession number :
edsair.doi...........7a1b6d16a5f436f3bae698e7ac5c323b
Full Text :
https://doi.org/10.1021/acs.joc.1c00817