Synthesis and Cytotoxicity of Novel 10-Substituted Dihydroartemisinin Derivatives Containing N-Arylphenyl-ethenesulfonamide Groups

Molecules

Yajing Liu¹  Zijian Liu¹  Jiyue Shi¹  Huimin Chen¹  Bin Mi¹  Peng Li¹ 

[1] id="af1-molecules-18-02864">Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, Chi

关键词: 10-substituted dihydroartemisinin derivatives;    synthesis;    anti-cancer;   

DOI  :  10.3390/molecules18032864

来源: mdpi

【 摘 要 】

The manuscript describes the synthesis of 10-substituted dihydroartemisinin derivatives containing N-aryl phenylethenesulfonamide groups and their in vitro anti-tumor activities against the HT-29, MDA-MB-231, U87MG, H460, A549 and HL-60 cancer cell lines and the normal WI-38 cell line. Most tested compounds showed enhanced cytotoxic activities and good selectivity toward the MDA-MB-231, HT-29 and HL-60 cell lines, with IC₅₀ values in the single-digit μM range as compared with dihydroartemisinin (DHA), and all of them displayed less toxicity towards WI-38 cells. Among them, compounds 3c and 6c with trifluoromethoxy groups on the N-phenyl ring were found to be most active compounds against the six tested cancer cell lines.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.