期刊
CANCER LETTERS
卷 183, 期 1, 页码 69-77出版社
ELSEVIER SCI IRELAND LTD
DOI: 10.1016/S0304-3835(02)00084-8
关键词
p53; HDM2; nonpeptidic small molecule HDM2 inhibitor
类别
Peptidic Mouse Double Minute (MDM2) inhibitors have been demonstrated to effectively inhibit the interaction between p53 and MDM2, thus providing a therapeutic strategy for some tumors. However, there is no report on non-peptidic inhibitors. In this study non-peptidic HDM2 (the human homologue of MDM2) inhibitors were obtained by computer-aided design and subsequently synthesized by chemical method. Bio-evaluation showed that some of these inhibitors have affinity with HDM2, and can cause death of some turner cells which express wild-type p53. Cellular assays showed that one of these compounds, syc-7, can activate the p53 pathway in some of these tumor cell lines, and further induce apoptosis. The results suggest that developing non-peptidic small-molecule HDM2 inhibitors is a promising way for new antitumor drug discovery. (C) 2002 Elsevier Science Ireland Ltd. All rights reserved.
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