title: Facile synthesis and anticancer activity of C-10 non-acetal deoxoartemisinin dimers.
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.
authors.affiliation: Department of Chemistry, Center for Innovation in Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai 50200, Thailand.
authors.forename: Supannee
authors.initials: S
authors.lastname: Phothongkam
authors.forename: Sirirat
authors.initials: S
authors.lastname: Chancharunee
authors.forename: Angkana
authors.initials: A
authors.lastname: Saovapakhiran
authors.forename: Uthai
authors.initials: U
authors.lastname: Wichai
authors.forename: Manat
authors.initials: M
authors.lastname: Pohmakotr
mesh_terms: D000080:Acetals / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D037621:Artemisinins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D018938:Caco-2 Cells; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D019281:Dimerization; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D000080:Acetals; D000970:Antineoplastic Agents; D037621:Artemisinins; C063801:deoxoartemisinin