Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives
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 ce...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2013-04-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/18/4/4158 |
| _version_ | 1831838904608620544 |
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| author | Taigang Liang Qingshan Li Chaoqun Yan Mengnan Hu Xue Du Luhui Ren |
| author_facet | Taigang Liang Qingshan Li Chaoqun Yan Mengnan Hu Xue Du Luhui Ren |
| author_sort | Taigang Liang |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-23T05:41:48Z |
| format | Article |
| id | doaj.art-c78ded6e55ae4b74a25bca638c0b1bdc |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-23T05:41:48Z |
| publishDate | 2013-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-c78ded6e55ae4b74a25bca638c0b1bdc2022-12-21T17:58:09ZengMDPI AGMolecules1420-30492013-04-011844158416910.3390/molecules18044158Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone DerivativesTaigang LiangQingshan LiChaoqun YanMengnan HuXue DuLuhui RenAn 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.http://www.mdpi.com/1420-3049/18/4/41584-methyl-(3'S,4'S)-cis-khellactone derivativesasymmetric synthesisantitumor activity |
| spellingShingle | Taigang Liang Qingshan Li Chaoqun Yan Mengnan Hu Xue Du Luhui Ren Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives Molecules 4-methyl-(3'S,4'S)-cis-khellactone derivatives asymmetric synthesis antitumor activity |
| title | Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives |
| title_full | Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives |
| title_fullStr | Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives |
| title_full_unstemmed | Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives |
| title_short | Design, Synthesis and Antitumor Activity of Novel 4-Methyl-(3'S,4'S)-cis-khellactone Derivatives |
| title_sort | design synthesis and antitumor activity of novel 4 methyl 3 039 s 4 039 s cis khellactone derivatives |
| topic | 4-methyl-(3'S,4'S)-cis-khellactone derivatives asymmetric synthesis antitumor activity |
| url | http://www.mdpi.com/1420-3049/18/4/4158 |
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