期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 98, 期 -, 页码 30-48出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.05.012
关键词
alpha-branched alpha,beta-unsaturated ketones; Antiproliferative activity; Cell cycle arrest; Apoptosis; QSAR; Granulocytic differentiation
资金
- European Social Fund under the Global Grant measure [VP1-3.1-SMM-07-K-01-002]
A series of alpha-branched alpha,beta-unsaturated ketones were prepared via boron trifluoride etherate mediated reaction between arylalkynes and carboxaldehydes. The evaluation of the antiproliferative activity over hematological (NB4) and solid cancer (A549, MCF-7) cell lines provided a structure-activity relationship. 5-Parameter QSAR equations were built which were able to explain 80%-92% of the variance in activity. The resulting selective lead compound showed IC50 value 0.6 mu M against the hematological cell line and did not cause apoptosis, but blocked cell cycle in G0/G1. Moreover, it was demonstrated that this compound enhances and accelerates retinoic acid induced granulocytic differentiation. (C) 2015 Published by Elsevier Masson SAS.
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