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Molecules 2013, 18(3), 2864-2877; doi:10.3390/molecules18032864
Article

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

, , , , ,  and *
Key Laboratory of Original New Drug Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
* Author to whom correspondence should be addressed.
Received: 4 December 2012 / Revised: 28 December 2012 / Accepted: 31 December 2012 / Published: 4 March 2013
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Abstract

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.
Keywords: 10-substituted dihydroartemisinin derivatives; synthesis; anti-cancer 10-substituted dihydroartemisinin derivatives; synthesis; anti-cancer
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Liu, Y.; Liu, Z.; Shi, J.; Chen, H.; Mi, B.; Li, P.; Gong, P. Synthesis and Cytotoxicity of Novel 10-Substituted Dihydroartemisinin Derivatives Containing N-Arylphenyl-ethenesulfonamide Groups. Molecules 2013, 18, 2864-2877.

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