Borrelidin analogues with antimalarial activity: Design,synthesis and biological evaluation against Plasmodium falciparum parasites |
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Authors: | Akihiro Sugawara Toshiaki Tanaka Tomoyasu Hirose Aki Ishiyama Masato Iwatsuki Yoko Takahashi Kazuhiko Otoguro Satoshi ōmura Toshiaki Sunazuka |
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Institution: | The Kitasato Institute and Kitasato Institute for Life Sciences and Graduate School of Infection Control Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan |
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Abstract: | Borrelidin, a structurally unique 18-membered macrolide, was found to express antimalarial activity against drug-resistant Plasmodium falciparum malaria parasites, with IC50 value of 0.93 ng/mL. However, it also displays strong cytotoxicity against human diploid embryonic MRC-5 cells. To investigate the issue of the cytotoxicity of borrelidin, borrelidin-based analogues were synthesized and their anti-Plasmodium properties were evaluated. In this communication, we report that a novel borrelidin analogue, bearing the CH2SPh moiety via a triazole linkage, was found to retain a potent antimalarial activity, against drug-sensitive and drug-resistant parasite strains, but possess only weak cytotoxicity against human cells. |
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