1429308-26-8Relevant articles and documents
Borrelidin analogues with antimalarial activity: Design, synthesis and biological evaluation against Plasmodium falciparum parasites
Sugawara, Akihiro,Tanaka, Toshiaki,Hirose, Tomoyasu,Ishiyama, Aki,Iwatsuki, Masato,Takahashi, Yoko,Otoguro, Kazuhiko,Omura, Satoshi,Sunazuka, Toshiaki
, p. 2302 - 2305 (2013/05/09)
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.