期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 122, 期 -, 页码 546-556出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.07.020
关键词
CDKs; Anticancer; Palbociclib; Synthesis
资金
- National Nature Science Foundation of China [81501529]
- Fundamental Research Funds for the Central Universities [2015PY001x]
A series of new palbociclib analogs by extensive functionalization of the tail piperazine ring with various carbamates and amides have been synthesized. All the palbociclib derivatives were evaluated for their cytotoxic activities against MCF-7 cell line. From the anti-proliferation activity results, two of the tested compounds (compounds 4d and 4e) showed significant cytotoxic effects. And compounds 4d and 4e exhibited potent anticancer activities in MDA-MB-453 and MDA-MB-231 cells. Among these derivatives compound 4e was found to possess cytotoxicity that is better than standard drug palbociclib. Moreover, compound 4e demonstrated robust tumor growth inhibition in vivo model. (C) 2016 Elsevier Masson SAS. All rights reserved.
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