Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells

Xuelin Yang; Wei Wang; Jun Tan; Dandan Song; Ming Li; Dan Liu; Yongkui Jing; Linxiang Zhao

doi:10.1016/j.bmcl.2009.05.076

Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4385-8. doi: 10.1016/j.bmcl.2009.05.076. Epub 2009 May 27.

Authors

Xuelin Yang¹, Wei Wang, Jun Tan, Dandan Song, Ming Li, Dan Liu, Yongkui Jing, Linxiang Zhao

Affiliation

¹ Shenyang Pharmaceutical University, Shenyang 110016, PR China.

PMID: 19501507
DOI: 10.1016/j.bmcl.2009.05.076

Abstract

Fifteen dihydroartemisinin derivatives containing a substituted chalcone linked by either ether or ester were synthesized and investigated for their cytotoxicity in human leukemia HL-60 and mouse lymphoma P388 cells. These derivatives have greater antiproliferative and cytotoxic effects in both cell lines than dihydroartemisinin. Dihydroartemisinin chalcones linked by ether are more cytotoxic than dihydroartemisinin chalcones linked by ester with apoptosis induction abilities.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology
Apoptosis
Artemisinins / chemical synthesis*
Artemisinins / pharmacology
Cell Line, Tumor
Cell Proliferation / drug effects
Chalcones / chemical synthesis*
Chalcones / chemistry
Chalcones / pharmacology
Chemistry, Pharmaceutical / methods
Drug Design
HL-60 Cells
Humans
Inhibitory Concentration 50
Leukemia / drug therapy*
Mice
Models, Chemical

Substances

Antineoplastic Agents
Artemisinins
Chalcones
artenimol