Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells
We have designed and synthesized 6 <i>ent</i>-Kaurane-type diterpenoid derivatives containing α,β-unsaturated ketone moieties. In vitro, activity was evaluated against three human tumor cell lines and a rat myogenic cell line (HepG2, NSCLC-H292, SNU-1040, L6) by MTT ass...
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MDPI AG
2018-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/23/12/3216 |
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| author | Yu Hu Xiao-Nian Li Ze-Jin Ma Pema-Tenzin Puno Yong Zhao Yan Zhao Ye-Zhi Xiao Wei Zhang Jing-Ping Liu |
| author_facet | Yu Hu Xiao-Nian Li Ze-Jin Ma Pema-Tenzin Puno Yong Zhao Yan Zhao Ye-Zhi Xiao Wei Zhang Jing-Ping Liu |
| author_sort | Yu Hu |
| collection | DOAJ |
| description | We have designed and synthesized 6 <i>ent</i>-Kaurane-type diterpenoid derivatives containing α,β-unsaturated ketone moieties. In vitro, activity was evaluated against three human tumor cell lines and a rat myogenic cell line (HepG2, NSCLC-H292, SNU-1040, L6) by MTT assay. All the tested compounds exhibited comparable or higher activity than DDP and eriocalyxin B. Compounds <b>16</b>, <b>17</b> and <b>18</b> are promising anti-tumor leads due to their cytotoxic potencies and higher selectivity, with SI values of 161.06, 47.80 and 128.20, respectively. |
| first_indexed | 2024-12-13T00:47:43Z |
| format | Article |
| id | doaj.art-71ae0ac0d02c4c50950c52382cdbd1cd |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-13T00:47:43Z |
| publishDate | 2018-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-71ae0ac0d02c4c50950c52382cdbd1cd2022-12-22T00:05:00ZengMDPI AGMolecules1420-30492018-12-012312321610.3390/molecules23123216molecules23123216Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor CellsYu Hu0Xiao-Nian Li1Ze-Jin Ma2Pema-Tenzin Puno3Yong Zhao4Yan Zhao5Ye-Zhi Xiao6Wei Zhang7Jing-Ping Liu8Department of Chemistry, Yunnan Normal University, Kunming 650092, ChinaState Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Kunming 650201, ChinaDepartment of Chemistry, Yunnan Normal University, Kunming 650092, ChinaState Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Kunming 650201, ChinaDepartment of Chemistry, Yunnan Normal University, Kunming 650092, ChinaDepartment of Chemistry, Yunnan Normal University, Kunming 650092, ChinaDepartment of Chemistry, Yunnan Normal University, Kunming 650092, ChinaDepartment of Chemistry, Yunnan Normal University, Kunming 650092, ChinaDepartment of Chemistry, Yunnan Normal University, Kunming 650092, ChinaWe have designed and synthesized 6 <i>ent</i>-Kaurane-type diterpenoid derivatives containing α,β-unsaturated ketone moieties. In vitro, activity was evaluated against three human tumor cell lines and a rat myogenic cell line (HepG2, NSCLC-H292, SNU-1040, L6) by MTT assay. All the tested compounds exhibited comparable or higher activity than DDP and eriocalyxin B. Compounds <b>16</b>, <b>17</b> and <b>18</b> are promising anti-tumor leads due to their cytotoxic potencies and higher selectivity, with SI values of 161.06, 47.80 and 128.20, respectively.https://www.mdpi.com/1420-3049/23/12/3216<i>ent</i>-kaurane-type diterpenoid derivativesantitumorsynthesis |
| spellingShingle | Yu Hu Xiao-Nian Li Ze-Jin Ma Pema-Tenzin Puno Yong Zhao Yan Zhao Ye-Zhi Xiao Wei Zhang Jing-Ping Liu Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells Molecules <i>ent</i>-kaurane-type diterpenoid derivatives antitumor synthesis |
| title | Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_full | Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_fullStr | Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_full_unstemmed | Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_short | Synthesis of Novel <i>ent</i>-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_sort | synthesis of novel i ent i kaurane type diterpenoid derivatives effective for highly aggressive tumor cells |
| topic | <i>ent</i>-kaurane-type diterpenoid derivatives antitumor synthesis |
| url | https://www.mdpi.com/1420-3049/23/12/3216 |
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