Synthesis and anticancer activities of 4-oxobenzopyrano[2,3-d]pyrimidines.
Hadfield, John A Pavlidis, V H Perry, P J McGown, Alan T
Hadfield, John A
Pavlidis, V H
Perry, P J
McGown, Alan T
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Abstract
Several 2-aryl-4-oxoxbenzopyrano[2,3-d]pyrimidines have previously been shown to exhibit in vivo antitumor activity in mice with P388 lymphocytic leukemia. In the present study, a series of novel substituted benzopyrano[2,3-d]pyrimidines have been prepared and tested for cytotoxic activity against a panel of cancer cell lines including the P388 lymphocytic leukemia cell line. The unsubstituted parent compound, some methoxylated derivatives and a cyclohexyl derivative all exhibited potent cytotoxic activity (IC50 values 0.3-0.64 microM). A number of derivatives, including the unsubstituted parent pyrimidine, were shown to cause a significant perturbation in cell cycle kinetics with an observed 2- to 3-fold increase in cells in the G2/M phase of the cell cycle. Furthermore, a polymethoxylated derivative, 2-(3,4,5-trimethoxyphenyl)-9-methoxy-4-oxo-2,3-dihydrobenzopyrano[ 2,3-d]pyrimidine 13, was shown to be selectively active against a number of human ovarian cell lines.
Description
Date
1999-07
Publisher
Collections
Keywords
Leukaemia P388
Ovarian Cancer
Cultured Tumour Cells
Ovarian Cancer
Cultured Tumour Cells
Type
Article
Citation
Synthesis and anticancer activities of 4-oxobenzopyrano[2,3-d]pyrimidines. 1999, 10 (6):591-5 Anticancer Drugs