Design, Synthesis and Antitumor Activity of Novel Artemisinin Derivatives Using Hybrid Approach
スポンサーリンク
概要
- 論文の詳細を見る
In an attempt to develop potent and selective anti-tumor agents, two novel series of artemisinin-chalcone hybrids were designed, synthesized and screened for their antitumor activities against HT-29, A549, MDA-MB-231, HeLa and H460 cell lines in vitro. Nearly all of the tested compounds showed significantly increased anti-tumor activity compared with the corresponding dihydroartemisinin (DHA). Most of the title compounds displayed good selectivity toward HT-29 and HeLa cell lines with IC50 values ranging from 0.09 to 0.85 μM. Among them, the most promising compound 9c (IC50 range of 0.09—0.93 μM) was 10.5- to 70-times more active than DHA (IC50 range of 5.6—15.6 μM) respectively.
著者
-
Zhai Xin
Key Lab Of New Drugs Design And Discovery Of Liaoning Province School Of Pharmaceutical Engineering
-
Ren Lixiang
Shenyang J & Health Bio-technic Dev. Co. Ltd.
-
Xie Lijun
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmace
-
Meng Haiyan
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmace
-
Liu Chun
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmace
-
Zhu Wufu
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmace
-
Zhao Yanfang
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmace
-
Zhu Wufu
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University
-
Zhu Wufu
Key Laboratory of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University
-
Ren Lixiang
Shenyang J & Health Bio-technic Development Co., Ltd.
-
Liu Chun
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University
-
Meng Haiyan
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University
関連論文
- Synthesis and Cytotoxicity Studies of Novel [1,2,4]Triazolo[1,5-a] pyrimidine-7-amines
- Design, Synthesis and Antitumor Activity of Novel Artemisinin Derivatives Using Hybrid Approach
- Design, Synthesis and Anticancer Activity of 4-Morpholinothieno[3,2-d]pyrimidine Derivatives Bearing Arylmethylene Hydrazine Moiety
- Design, Synthesis and Cytotoxicity of Novel 2-Arylvinyl-4-aminoquinoline Derivatives
- Design, Synthesis and Anticancer Activities of Diaryl Urea Derivatives Bearing N-Acylhydrazone Moiety