title: Design, synthesis and antitumor activity of novel 4-methyl-(3'S,4'S)-cis-khellactone derivatives.
abstract: An asymmetric synthesis of a series of novel 4-methyl-(3'S,4'S)-cis-khellactone derivatives 3a-o is reported for the first time. Their structures were confirmed by 1H-NMR, 13C-NMR and MS. Their cytotoxic activity was evaluated by the MTT assay against three selected human cancer cell lines: HEPG-2 (human liver carcinoma), SGC-7901 (human gastric carcinoma), LS174T (human colon carcinoma). Some compounds showed high inhibitory activity against these human cancer cell lines. Among them, compound 3a exhibited strong cytotoxicity, with IC50 values ranging from 8.51 to 29.65 μM. The results showed that 4-methyl-cis-khellactone derivatives with S,S configuration could be a potential antitumor agents.
authors.affiliation: School of Pharmaceutical Science, Shanxi Medical University, No 56, Xinjian Nan Road, Taiyuan 030001, Shanxi, China. renluhui@126.com
authors.forename: Luhui
authors.initials: L
authors.lastname: Ren
authors.forename: Xue
authors.initials: X
authors.lastname: Du
authors.forename: Mengnan
authors.initials: M
authors.lastname: Hu
authors.forename: Chaoqun
authors.initials: C
authors.lastname: Yan
authors.forename: Taigang
authors.initials: T
authors.lastname: Liang
authors.forename: Qingshan
authors.initials: Q
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: C583740:4-methyl-(3'S,4'S)-cis-khellactone; D000970:Antineoplastic Agents; D003374:Coumarins