Title of article :
Design, syntheses, and antitumor activity of novel chromone and aurone derivatives Original Research Article
Author/Authors :
Wei Huang، نويسنده , , Ming-Zhen Liu، نويسنده , , Yan Li، نويسنده , , Ying Tan، نويسنده , , Guangfu Yang، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2007
Pages :
7
From page :
5191
To page :
5197
Abstract :
A series of new chromone analogues bearing heterocyclic thioether moiety and aurone analogues bearing cyclic tertiary amine moiety were designed and synthesized under microwave irradiation. The synthetic protocol was found to present many advantages, such as higher yields, shorter reaction time (10–20 min), mild condition, and readily isolation of the products. The synthesized compounds were assayed for their antitumor activity against four kinds of human solid tumor cell lines including HCCLM-7, Hep-2, MDA-MB-435S, and SW-480. Two compounds, (Z)-2-((4-benzyl-piperazin-1-yl)methylene)benzofuran-3(2H)-one 5e and (Z)-2-((4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)methylene)benzofuran-3(2H)-one 5f, were identified as the most promising candidates with the IC50 values in the range of 4.1–13.1 μM. Further cell cycle studies revealed that compounds 5e and 5f arrest the cell cycle in G0/G1 phase and displayed apoptosis-inducing effect on Hep-2 cells.
Keywords :
MAO inhibitors , Amphetamine derivatives , Monoamine oxidase , molecular dynamics simulation
Journal title :
Bioorganic and Medicinal Chemistry
Serial Year :
2007
Journal title :
Bioorganic and Medicinal Chemistry
Record number :
1305923
Link To Document :
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