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

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7598-601. doi: 10.1016/j.bmcl.2012.10.020.

Supannee Phothongkam ¹, Sirirat Chancharunee, Angkana Saovapakhiran, Uthai Wichai, Manat Pohmakotr

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Affiliation

1 Department of Chemistry, Center for Innovation in Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai 50200, Thailand.

PMID: 23103096 DOI: 10.1016/j.bmcl.2012.10.020

Abstract

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.

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