Antimitotic activity of diaryl compounds with structural features resembling combretastatin A-4.
Aleksandrzak, Krzysztof ; McGown, Alan T ; Hadfield, John A
Aleksandrzak, Krzysztof
McGown, Alan T
Hadfield, John A
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Abstract
Series of diaryl ethers, amines and amides have been synthesized and tested for antitumor activity. These diaryl compounds possess some of the structural features of combretastatin A-4 (a potent antimitotic agent). They were designed to discover whether transferring these structural motifs from stilbenes to heterosubstituted diaryl compounds would enhance their biochemical activities. Molecular modeling studies suggested that these diaryl compounds could adopt conformations similar to combretastatin A-4. However, although some agents (5-7) were cytotoxic and others (10 and 12) could interact with tubulin, none were as potent as combretastatin A-4.
Description
Date
1998-07
Publisher
Collections
Keywords
Antitumour Drug Screening Assays
Leukaemia P388
Cultured Tumour Cells
Leukaemia P388
Cultured Tumour Cells
Type
Article
Citation
Antimitotic activity of diaryl compounds with structural features resembling combretastatin A-4. 1998, 9 (6):545-50 Anticancer Drugs