Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents.

Authors :: Li S
Li G
Yang X
Meng Q
Yuan S
He Y
Sun D
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Jul 15; Vol. 28 (13), pp. 2275-2278. Date of Electronic Publication: 2018 May 17.
Publication Year :: 2018
Abstract: Ten novel artemisinin derivatives containing fluorine atoms were synthesized and their structures were confirmed by <superscript>1</superscript> H NMR, <superscript>13</superscript> C NMR and HRMS technologies in this study. The in vitro cytotoxicity against U87MG, SH-SY5Y, MCF-7, MDA-MB-231, A549 and A375 cancer cell lines was evaluated by MTT assay. Compound 9j was the most potent anti-proliferative agent against the human breast cancer MCF-7 cells (IC <subscript>50</subscript>  = 2.1 μM). The mechanism of action of compound 9j was further investigated by analysis of cell apoptosis and cell cycle. Compound 9j induced cell apoptosis and arrested cell cycle at G1 phase in MCF-7 cells. Our promising findings indicated that the compound 9j could stand as potential lead compound for further investigation.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)

Subjects :: Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Apoptosis drug effects
Artemisinins chemical synthesis
Artemisinins chemistry
Cell Line, Tumor
Drug Design
Drug Screening Assays, Antitumor
G1 Phase Cell Cycle Checkpoints drug effects
Humans
Molecular Structure
Antineoplastic Agents pharmacology
Artemisinins pharmacology
Fluorine chemistry

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