Capela, RitaOliveira, RudiGoncalves, Lidia M.Domingos, AnaGut, JiriRosenthal, Philip J.Lopes, FranciscaMoreira, Rui2015-12-302015-12-302009BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 19, n. 12 (2009), p. 3229-32320960-894Xhttp://hdl.handle.net/10451/21198A series of artemisinin-vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates were active against the Plasmodium falciparum W2 strain in the low nanomolar range and those containing the Leu-hPhe core inhibited falcipain-2 in low micromolar range. (C) 2009 Elsevier Ltd. All rights reserved.. - FCT (Portugal) [SFRH/BD/30418/2006]; National Institutes of Health. - This work was supported by FCT (Portugal) and the National Institutes of Health; R. C. acknowledges FCT for the PhD grant SFRH/BD/30418/2006. PJR is a Doris Duke Charitable Foundation Distinguished Clinical Scientist.application/pdfengChemistry, MedicinalChemistry, Organicjournal articlehttp://dx.doi.org/10.1016/j.bmcl.2009.04.100