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Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells
We have designed and synthesized 6 ent-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 exhibite...
| Autores principales: | , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2018
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321055/ https://www.ncbi.nlm.nih.gov/pubmed/30563165 http://dx.doi.org/10.3390/molecules23123216 |
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| author | Hu, Yu Li, Xiao-Nian Ma, Ze-Jin Puno, Pema-Tenzin Zhao, Yong Zhao, Yan Xiao, Ye-Zhi Zhang, Wei Liu, Jing-Ping |
| author_facet | Hu, Yu Li, Xiao-Nian Ma, Ze-Jin Puno, Pema-Tenzin Zhao, Yong Zhao, Yan Xiao, Ye-Zhi Zhang, Wei Liu, Jing-Ping |
| author_sort | Hu, Yu |
| collection | PubMed |
| description | We have designed and synthesized 6 ent-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 16, 17 and 18 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. |
| format | Online Article Text |
| id | pubmed-6321055 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2018 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-63210552019-01-14 Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells Hu, Yu Li, Xiao-Nian Ma, Ze-Jin Puno, Pema-Tenzin Zhao, Yong Zhao, Yan Xiao, Ye-Zhi Zhang, Wei Liu, Jing-Ping Molecules Article We have designed and synthesized 6 ent-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 16, 17 and 18 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. MDPI 2018-12-05 /pmc/articles/PMC6321055/ /pubmed/30563165 http://dx.doi.org/10.3390/molecules23123216 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
| spellingShingle | Article Hu, Yu Li, Xiao-Nian Ma, Ze-Jin Puno, Pema-Tenzin Zhao, Yong Zhao, Yan Xiao, Ye-Zhi Zhang, Wei Liu, Jing-Ping Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title | Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_full | Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_fullStr | Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_full_unstemmed | Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_short | Synthesis of Novel ent-Kaurane-Type Diterpenoid Derivatives Effective for Highly Aggressive Tumor Cells |
| title_sort | synthesis of novel ent-kaurane-type diterpenoid derivatives effective for highly aggressive tumor cells |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321055/ https://www.ncbi.nlm.nih.gov/pubmed/30563165 http://dx.doi.org/10.3390/molecules23123216 |
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