期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 124, 期 -, 页码 840-851出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.09.013
关键词
[1,2]Oxazolo[5,4-e]isoindoles; alpha-hydroxyalkyl ketones; Antitubulin agents; Diffuse malignant peritoneal mesothelioma
资金
- Ministero dell'Istruzionedell'Universita e della Ricerca (MIUR)
- AIRC fellowship [16360]
A series of [1,2]Oxazolo [5,4-e]isoindoles has been synthesized through a versatile and high yielding sequence. All the new structures showed in the (HNMR)-H-1 spectra, the typical signal in the 834-8.47 ppm attributable to the H-3 of the [1,2]oxazole moiety. Among all derivatives, methoxy benzyl substituents at positions 3 and 4 or/and 5 were very effective in reducing the growth of different tumor cell lines, including diffuse malignant peritoneal mesothelioma (DMPM), an uncommon and rapidly malignancy poorly responsive to available therapeutic options. The most active compound 6j was found to impair tubulin polymerization, cause cell cycle arrest at G2/M phase and induce apoptosis in DMPM cells, making it as a new lead for the discovery of new potent antimitotic drugs. (C) 2016 Elsevier Masson SAS. All rights reserved.
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