Synthesis and biological activities of novel artemisinin derivatives as cysteine protease falcipain-2 inhibitors

Yang Liu; Wei Qiang Lu; Kun Qiang Cui; Wei Luo; Jian Wang; Chun Guo

doi:10.1007/s12272-012-0902-4

Synthesis and biological activities of novel artemisinin derivatives as cysteine protease falcipain-2 inhibitors

Yang Liu, Wei Qiang Lu, Kun Qiang Cui, Wei Luo, Jian Wang, Chun Guo

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	1525-1531
Number of pages	7
Journal	Archives of Pharmacal Research
Volume	35
Issue number	9
DOIs	https://doi.org/10.1007/s12272-012-0902-4
State	Published - Sep 2012
Externally published	Yes

Keywords

(thio)Semicarbazone derivatives
Antimalarial
Artemisinin derivatives
Falcipain-2 inhibitor
Inhibition activity
Synthesis

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10.1007/s12272-012-0902-4

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abstract = "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.",

keywords = "(thio)Semicarbazone derivatives, Antimalarial, Artemisinin derivatives, Falcipain-2 inhibitor, Inhibition activity, Synthesis",

author = "Yang Liu and Lu, \{Wei Qiang\} and Cui, \{Kun Qiang\} and Wei Luo and Jian Wang and Chun Guo",

year = "2012",

month = sep,

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T1 - Synthesis and biological activities of novel artemisinin derivatives as cysteine protease falcipain-2 inhibitors

AU - Liu, Yang

AU - Lu, Wei Qiang

AU - Cui, Kun Qiang

AU - Luo, Wei

AU - Wang, Jian

AU - Guo, Chun

PY - 2012/9

Y1 - 2012/9

N2 - 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.

AB - 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.

KW - (thio)Semicarbazone derivatives

KW - Antimalarial

KW - Artemisinin derivatives

KW - Falcipain-2 inhibitor

KW - Inhibition activity

KW - Synthesis

UR - https://www.scopus.com/pages/publications/84872106504

U2 - 10.1007/s12272-012-0902-4

DO - 10.1007/s12272-012-0902-4

M3 - 文章

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AN - SCOPUS:84872106504

SN - 0253-6269

VL - 35

SP - 1525

EP - 1531

JO - Archives of Pharmacal Research

JF - Archives of Pharmacal Research

IS - 9

ER -

Synthesis and biological activities of novel artemisinin derivatives as cysteine protease falcipain-2 inhibitors

Abstract

Keywords

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