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

Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells

1email, 2email, 3email, 1email, 1,* email and 1,* email
Received: 27 April 2013; in revised form: 15 May 2013 / Accepted: 16 May 2013 / Published: 21 May 2013
(This article belongs to the Section Medicinal Chemistry)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: 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
PDF Full-text Download PDF Full-Text [268 KB, uploaded 18 June 2014 20:05 CEST]

Export to BibTeX |
EndNote


MDPI and ACS Style

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.

AMA Style

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(5):5980-5992.

Chicago/Turabian Style

Ma, Wei-Wei; Shi, Qian-Qian; Ding, Ya-Hui; Long, Jing; Zhang, Quan; Chen, Yue. 2013. "Synthesis of Micheliolide Derivatives and Their Activities against AML Progenitor Cells." Molecules 18, no. 5: 5980-5992.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert