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

Kiyosei Takasu; Hiroshi Inoue; Hye Sook Kim; Makoto Suzuki; Tadao Shishido; Yusuke Wataya; Masataka Ihara

doi:10.1021/jm0155704

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

Kiyosei Takasu, Hiroshi Inoue, Hye Sook Kim, Makoto Suzuki, Tadao Shishido, Yusuke Wataya, Masataka Ihara

Research output: Contribution to journal › Article › peer-review

61 Citations (Scopus)

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 EC₅₀ values against P. falciparum in vitro in the range of 4-300 nM. Several compounds in this series have remarkable selective toxicity profiles (> 100).

Original language	English
Pages (from-to)	995-998
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	45
Issue number	5
DOIs	https://doi.org/10.1021/jm0155704
Publication status	Published - Feb 28 2002

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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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 EC50 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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AU - Takasu, Kiyosei

AU - Inoue, Hiroshi

AU - Kim, Hye Sook

AU - Suzuki, Makoto

AU - Shishido, Tadao

AU - Wataya, Yusuke

AU - Ihara, Masataka

PY - 2002/2/28

Y1 - 2002/2/28

N2 - 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 EC50 values against P. falciparum in vitro in the range of 4-300 nM. Several compounds in this series have remarkable selective toxicity profiles (> 100).

AB - 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 EC50 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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Rhodacyanine dyes as antimalarials. 1. Preliminary evaluation of their activity and toxicity

Abstract

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