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Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives

School of Pharmaceutical Science, Shanxi Medical University, No 56, Xinjian Nan Road, Taiyuan 030001, Shanxi, China
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These authors contributed equally to this work.
Molecules 2013, 18(4), 4158-4169; https://doi.org/10.3390/molecules18044158
Received: 16 February 2013 / Revised: 27 March 2013 / Accepted: 2 April 2013 / Published: 8 April 2013
An asymmetric synthesis of a series of novel 4-methyl-(3'S,4'S)-cis-khellactone derivatives 3ao 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. View Full-Text
Keywords: 4-methyl-(3'S,4'S)-cis-khellactone derivatives; asymmetric synthesis; antitumor activity 4-methyl-(3'S,4'S)-cis-khellactone derivatives; asymmetric synthesis; antitumor activity
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Ren, L.; Du, X.; Hu, M.; Yan, C.; Liang, T.; Li, Q. Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives. Molecules 2013, 18, 4158-4169.

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