Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells
Micheliolide (MCL) derivatives with etherification or esterification of the hydroxyl group at the C4 position were synthesized and evaluated for their activities against different acute myelogenous leukemia (AML) cell lines. These derivatives demonstrated comparable activities against AML cell lines...
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MDPI AG
2013-05-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/18/5/5980 |
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| author | Yue Chen Quan Zhang Jing Long Qian-Qian Shi Ya-Hui Ding Wei-Wei Ma |
| author_facet | Yue Chen Quan Zhang Jing Long Qian-Qian Shi Ya-Hui Ding Wei-Wei Ma |
| author_sort | Yue Chen |
| collection | DOAJ |
| description | Micheliolide (MCL) derivatives with etherification or esterification of the hydroxyl group at the C4 position were synthesized and evaluated for their activities against different acute myelogenous leukemia (AML) cell lines. These derivatives demonstrated comparable activities against AML cell lines HL-60 and doxorubicin resistant cell line HL-60/A. As to multi-drug resistant AML progenitor cells KG-1a, MCL and some of its derivatives maintained significant activities, and only 1.1–2.7 fold activity reductions were observed when compared with the activities against HL-60, while doxorubicin showed 20-fold activity reduction. Our study demonstrated that the C4 hydroxyl group of MCL might not only be a suitable position for structural modifications, but also be a starting point for the design of appropriate molecular probes to explore the specific targets in the progenitor cell line KG-1a. |
| first_indexed | 2024-12-10T15:02:11Z |
| format | Article |
| id | doaj.art-abccfd70e5e54d7dac062306bbca96e4 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-10T15:02:11Z |
| publishDate | 2013-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-abccfd70e5e54d7dac062306bbca96e42022-12-22T01:44:09ZengMDPI AGMolecules1420-30492013-05-011855980599210.3390/molecules18055980Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor CellsYue ChenQuan ZhangJing LongQian-Qian ShiYa-Hui DingWei-Wei MaMicheliolide (MCL) derivatives with etherification or esterification of the hydroxyl group at the C4 position were synthesized and evaluated for their activities against different acute myelogenous leukemia (AML) cell lines. These derivatives demonstrated comparable activities against AML cell lines HL-60 and doxorubicin resistant cell line HL-60/A. As to multi-drug resistant AML progenitor cells KG-1a, MCL and some of its derivatives maintained significant activities, and only 1.1–2.7 fold activity reductions were observed when compared with the activities against HL-60, while doxorubicin showed 20-fold activity reduction. Our study demonstrated that the C4 hydroxyl group of MCL might not only be a suitable position for structural modifications, but also be a starting point for the design of appropriate molecular probes to explore the specific targets in the progenitor cell line KG-1a.http://www.mdpi.com/1420-3049/18/5/5980leukemia progenitor cellmicheliolideKG-1aderiviativesythesis |
| spellingShingle | Yue Chen Quan Zhang Jing Long Qian-Qian Shi Ya-Hui Ding Wei-Wei Ma Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells Molecules leukemia progenitor cell micheliolide KG-1a deriviative sythesis |
| title | Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells |
| title_full | Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells |
| title_fullStr | Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells |
| title_full_unstemmed | Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells |
| title_short | Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells |
| title_sort | synthesis of micheliolide derivatives and their activities against aml progenitor cells |
| topic | leukemia progenitor cell micheliolide KG-1a deriviative sythesis |
| url | http://www.mdpi.com/1420-3049/18/5/5980 |
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