Synthesis and biological evaluation of antimalarial and antileukemic activity of new C-10 modified artemisinin derivatives

Abstract Several non-acetal artemisinin derivatives were synthesized and their antimalarial activity against chloroquine-resistant parasites as well as their antileukemic activity were investigated. The azide 10 was proved to have slightly better activity than the current antimalarial drugs such as artesunate and chloroquine. In addition, the azide 10 and the aldehyde 7 were found to be effective in decreasing cell proliferation in leukemia cells.

Total Synthesis and Biological Investigation of (−)‐Artemisinin: The Antimalarial Activity of Artemisinin Is not Stereospecific

Here, we describe an efficient and diversity-oriented entry to both (-)-artemisinin (1) and its natural antipode (+)-artemisinin, starting from commercially and readily available S-(+)- and R-(-)-citronellene, respectively. Subsequently, we answered the still open question regarding the specificity of artemisinins action. By using a drug-sensitive Plasmodium falciparum NF54 strain, we showed that the antimalarial activity of artemisinin is not stereospecific. Our straightforward and biomimetic approach to this natural endoperoxide enables the synthesis of artemisinin derivatives that are not accessible through applying current methods and may help to address the problem of emerging resistan…

Totalsynthese und Untersuchung der biologischen Aktivität von (−)‐Artemisinin – die Antimalaria‐Aktivität von Artemisinin ist nicht stereospezifisch