Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin

Novel amide derivatives of non-acetal deoxoartemisinin were synthesized. Some of the derivatives had potent in vitro anticancer activity and the deoxoartemisinin amide trimer had potent in vivo antiangiogenic activity. Novel amide derivatives of C-12 non-acetal deoxoartemisinin were synthesized. Som...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-11, Vol.19 (22), p.6303-6306
Main Authors: Jung, Mankil, Park, Namsoo, Moon, Hyung-In, Lee, Yongnam, Chung, Won-Yoon, Park, Kwang-Kyun
Format: Article
Language:English
Subjects:
Acetals - chemistry
Amides - chemical synthesis
Amides - chemistry
Animals
Antiangiogenesis
Anticancer activity
Antineoplastic agents
Apoptosis - drug effects
Apoptosis - physiology
Artemisinins - chemical synthesis
Artemisinins - chemistry
Biological and medical sciences
Cell Proliferation
Deoxoartemisinin
Drug Design
Drug Screening Assays, Antitumor - methods
Endothelium, Vascular - drug effects
Endothelium, Vascular - pathology
General aspects
Humans
Inhibitory Concentration 50
Medical sciences
Mice
Mice, Nude
Neoplasm Transplantation
Non-acetal type
Pharmacology. Drug treatments
Structure-Activity Relationship
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Summary:Novel amide derivatives of non-acetal deoxoartemisinin were synthesized. Some of the derivatives had potent in vitro anticancer activity and the deoxoartemisinin amide trimer had potent in vivo antiangiogenic activity. Novel amide derivatives of C-12 non-acetal deoxoartemisinin were synthesized. Some of the derivatives had potent in vitro anticancer activity against major human cancer cell lines. The deoxoartemisinin amide trimer had potent in vivo antiangiogenic activity, according to the mouse matrigel plug assay.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.09.093