期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 115, 期 -, 页码 141-147出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.03.039
关键词
Spiropyrazolone; Antitumor; Cancer cell apoptosis; Structure-activity relationship
资金
- 863 Hi-Tech Program of China [2014AA020525]
- National Natural Science Foundation of China [81222044]
- National Basic Research Program of China [2014CB541800]
- Shanghai ShuGuang Project [14SG33]
Phenotypic screening of high quality compound library is an effective strategy to discover novel bioactive molecules. Previously, we developed the divergent organocatalytic cascade approach to efficiently construct a focused library with scaffold diversity and successfully identified a novel spiropyrazolone antitumor scaffold. Herein, a series of spiropyrazolone derivatives were designed, synthesized and assayed. Most of them showed good in vitro antitumor activity with a broad spectrum. Preliminary structure-activity relationship for the substitutions and the stereo configuration were obtained. Compound 5k showed good antitumor activity and could effectively induce cancer cell apoptosis, which represents a good starting point for the development of novel antitumor agents. (C) 2016 Elsevier Masson SAS. All rights reserved.
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