1254986-46-3Relevant academic research and scientific papers
Design, synthesis, and development of novel guaianolide-endoperoxides as potential antimalarial agents
Sun, Lingzhi,Shah, Falgun,Helal, Mohamed A.,Wu, Yunshan,Pedduri, Yakambram,Chittiboyina, Amar G.,Gut, Jiri,Rosenthal, Philip J.,Avery, Mitchell A.
supporting information; experimental part, p. 7864 - 7868 (2011/01/12)
Design and synthesis of a guaianolide-endoperoxide (thaperoxide) 3 was pursued as a new antimalarial lead which was found to be noncytotoxic as compared to the natural product lead thapsigargin 2. Several analogues of 3 were successfully synthesized and found to be comparable to derivatives of artemisinin 1 in in vitro antimalarial assay. Among the synthesized compounds, 22 showed excellent in vitro potency against the cultured parasites (W2 IC 50 = 13 nM) without apparent cytotoxicity. Furthermore, SAR trends in thaperoxide analogues are presented and explained with the help of docking studies in the homology model of PfSERCA(PfATP6).
