Facile synthesis and anticancer activity of C-10 non-acetal deoxoartemisinin dimers

In this research, N-(2-aminoethyl)glycine-linked C-10 non-acetal deoxoartemisinin dimers were synthesized by using solution phase peptide synthesis approach. In addition, chemical modification of the C-10 non-acetal deoxoartemisinin monomers and dimers by adding a lysine unit to the N-terminus has b...

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Bibliographic Details
Main Authors: Phothongkam S., Chancharunee S., Saovapakhiran A., Wichai U., Pohmakotr M.
Format: Article
Published: Elsevier Limited 2015
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Online Access:http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84870236110&origin=inward
http://cmuir.cmu.ac.th/handle/6653943832/38648
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Institution: Chiang Mai University
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Summary:In this research, N-(2-aminoethyl)glycine-linked C-10 non-acetal deoxoartemisinin dimers were synthesized by using solution phase peptide synthesis approach. In addition, chemical modification of the C-10 non-acetal deoxoartemisinin monomers and dimers by adding a lysine unit to the N-terminus has been performed. The biological activities of all synthesized compounds were evaluated against the colon cancer cell line (Caco-2). The non-acetal deoxoartemisinin monomers 12a, 15a-c and dimers 13a, 16a-c were active against Caco-2 cells and more potent than dihydroartemisinin. © 2012 Elsevier Ltd. All rights reserved.