Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity

  • J Med Chem. 2002 Feb 28;45(5):995-8. doi: 10.1021/jm0155704.
Kiyosei Takasu  1 ,  Hiroshi Inoue ,  Hye-Sook Kim ,  Makoto Suzuki ,  Tadao Shishido ,  Yusuke Wataya ,  Masataka Ihara
Affiliations
  • 1. Department of Organic Chemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Aobayama, Sendai 980-8578, Japan. [email protected]
PMID: 11855978 DOI: 10.1021/jm0155704
Abstract

The rhodacyanine dye MKT-077 (1), a potent antitumor agent, was found to possess strong in vitro activity against Plasmodium falciparum and a low cytotoxicity. Several new rhodacyanine dyes related to 1, containing a variety of linked heterocyclic moieties, were synthesized, and their antimalarial potencies were evaluated. The synthetic rhodacyanines were found to have EC(50) values against P. falciparum in vitro in the range of 4-300 nM. Several compounds in this series have remarkable selective toxicity profiles (>100).