New efficient artemisinin derived agents against human leukemia cells, human cytomegalovirus and Plasmodium falciparum: 2nd generation 1,2,4-trioxane-ferrocene hybrids

Highly potent artemisinin-derived dimers and trimers: Synthesis and evaluation of their antimalarial, antileukemia and antiviral activities

“…Connecting these precursors chemically with one or more other natural product fragments lead to the formation of hybrid compounds. [19][20][21][22][23][24][25][26][27][28][29][30] These hybrids often possess strikingly improved or new biological activities compared to their parent compounds. Although none of these hybrids have reached clinical application yet, there are many examples available in literature with already very promising in vivo results demonstrating the great potential of the hybridization concept.…”

Facile access to potent antiviral quinazoline heterocycles with fluorescence properties via merging metal-free domino reactions

“…Prevention and clinical interventions for HCMV disease are limited, since cross-resistance to all approved anti-HCMV drugs is increasingly observed31. As alternatives to standard drugs2332, our ongoing search for highly active hybrid molecules333435, which exceed their parent compounds in activity against HCMV, resulted in synthesis of new artesunic acid–quinazoline hybrids 8 and 9 (Fig. 7a and Supplementary Methods).…”

“…6) as coupling partners, since their fluorescence properties were considered beneficial for biological investigations. Artesunic acid on the other hand was selected because it proved to be a valuable building block in order to get highly bioactive compounds with just a few chemical transformations and also because of its promising pharmacological properties233235.…”

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

“…Anschließend wurde das Derivat 6 mit LiAlH 4 in THF quantitativ zum Allylalkohol 7 umgesetzt. [32] Dabei wurden zwar Unterschiede in der Zytotoxizitätg egen die l-6-Zellen festgestellt, allerdings war die Zytotoxizitätg egen CCRF-CEMund CEM/ADR5000-Zellen nahezu identisch. Während das Derivat 11 als E/Z-Gemisch (3:2) erhalten wurde, lag 12 als reines E-Isomer vor.D ie Reduktion des cis-anellierten, a,b-ungesättigten Esters 11 mit NiCl 2 /NaBH 4 in Methanol lieferte Derivat 13 in fast quantitativer Ausbeute und akzeptabler Diastereoselektivität( d.r.…”