Synthesis and biological activities of novel artemisinin derivatives as cysteine protease falcipain-2 inhibitors
A series of novel artemisinin derivatives were synthesized from artemisinin and different anilines. All compounds were obtained as β-isomers. The target compounds were evaluated for inhibition activity against Plasmodium falciparum falcipain-2 in vitro, and most of them exhibited potent inhibition in the low micromolar range and proved to be new types of falcipain-2 inhibitors.
Liu, Yang,Lu, Wei-Qiang,Cui, Kun-Qiang,Luo, Wei,Wang, Jian,Guo, Chun
p. 1525 - 1531
(2013/03/14)
Synthesis and structure-activity evaluation of isatin-β- thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein
Cancer multidrug resistance (MDR) mediated by ATP-binding cassette (ABC) transporters presents a significant unresolved clinical challenge. One strategy to resolve MDR is to develop compounds that selectively kill cells overexpressing the efflux transport
Hall, Matthew D.,Brimacombe, Kyle R.,Varonka, Matthew S.,Pluchino, Kristen M.,Monda, Julie K.,Li, Jiayang,Walsh, Martin J.,Boxer, Matthew B.,Warren, Timothy H.,Fales, Henry M.,Gottesman, Michael M.
experimental part
p. 5878 - 5889
(2011/10/08)
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