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Molecules 2013, 18(5), 5980-5992; doi:10.3390/molecules18055980

Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells

1,*  and 1,*
1 College of Pharmacy, the State Key Laboratory of Elemento-Organic Chemistry, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300071, China 2 College of Food Engineering and Biotechnology, Tianjin University of Science and Technology, Tianjin 300457, China 3 Accendatech Co., Ltd, Tianjin 300384, China
* Authors to whom correspondence should be addressed.
Received: 27 April 2013 / Revised: 15 May 2013 / Accepted: 16 May 2013 / Published: 21 May 2013
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: leukemia progenitor cell; micheliolide; KG-1a; deriviative; sythesis leukemia progenitor cell; micheliolide; KG-1a; deriviative; sythesis
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Ma, W.-W.; Shi, Q.-Q.; Ding, Y.-H.; Long, J.; Zhang, Q.; Chen, Y. Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells. Molecules 2013, 18, 5980-5992.

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