Each diastereomer of 10-thiophenyl-and 10-benzenesulfonyl-dihydroartemisinin was synthesized from artemisinin in three steps, and screened against chloroquine-resistance and chloroquine-sensitive Plasmodium falciparum. Three of the four tested compounds were found to be effective. Especially, 10β-benzenesulfonyl-dihydroartemisinin showed stronger antimalarial activity than artemisinin.
Synthesis of Diethylamino-Curcumin Mimics with Substituted Triazolyl Groups and Their Sensitization Effect of TRAIL Against Brain Cancer Cells. -A new curcumin mimic library (III) is synthesized using the Huisgen cycloaddition of alkynes with azide (I). The novel library is found to effectively stimulate the cytotoxicity of TRAIL, causing mild cytotoxicity when administered alone. In particular, compounds (IIIa), (IIIc), (IIIe), and (IIIf) are promising TRAIL-sensitizers with potential for application in combination chemotherapy of brain tumors. -(AHN, Y.; OH, S.; LEE, S. J.; PARK, B.-G.; PARK, Y.-S.; SHIN, W.-S.; JANG, H. J.; PARK, J. H.; KWON, D.; LEE*, S.; Bioorg. Med. Chem. Lett. 24 (2014) 15, 3346-3350, http://dx.
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