Rhodacyanine Dyes as Antimalarials. 1. Preliminary Evaluation of Their Activity and Toxicity
Journal of Medicinal Chemistry2002Vol. 45(5), pp. 995–998
Citations Over TimeTop 14% of 2002 papers
Kiyosei Takasu, Hiroshi Inoue, Hye‐Sook Kim, Makoto Suzuki, Tadao Shishido, Yusuke Wataya, Masataka Ihara
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).
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