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.
Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Yang
Y
Liu
Wei-Qiang
WQ
Lu
Kun-Qiang
KQ
Cui
Wei
W
Luo
Jian
J
Wang
Chun
C
Guo
D000814:Aniline Compounds / Q000737:chemistry; D000962:Antimalarials / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D037621:Artemisinins / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D020134:Catalytic Domain / Q000187:drug effects; D003546:Cysteine Endopeptidases / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D015853:Cysteine Proteinase Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D015195:Drug Design; D009682:Magnetic Resonance Spectroscopy; D062105:Molecular Docking Simulation; D009994:Osmolar Concentration; D010963:Plasmodium falciparum / Q000201:enzymology; D011485:Protein Binding; D017433:Protein Structure, Secondary / Q000187:drug effects; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors / Q000737:chemistry / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013882:Thiosemicarbazones / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D044366:Transition Temperature
D000814:Aniline Compounds; D000962:Antimalarials; D037621:Artemisinins; D015853:Cysteine Proteinase Inhibitors; D015800:Protozoan Proteins; D011994:Recombinant Proteins; D013882:Thiosemicarbazones; C031327:artemisinin; D003546:Cysteine Endopeptidases; C416224:falcipain 2