Synthesis and Antineoplastic Evaluation of Novel Unsymmetrical 1,3,4-Oxadiazoles.
作者： Valentina Nieddu , Giansalvo Pinna , Irene Marchesi , Luca Sanna , Battistina Asproni
DOI: 10.1021/ACS.JMEDCHEM.6B00468
关键词:
摘要: A series of novel 1,3,4-oxadiazoles was synthesized and evaluated for their cytotoxic activity in vitro tumor models. Four the new compounds (2d, 2j, 2k, 2n) showed growth inhibition XTT dye assay. The most active agent, high potency against human cancer cells with IC50s ranging from 0.05 to 1.7 μM. Preliminary SAR correlations suggested that nature chains on oxadiazole is important antitumor vitro. Compound 2j determined a G2/M arrest cell cycle also activated strong apoptotic response. β-tubulin immunofluorescence analysis indicated compound effectively inhibited microtubule organization all lines, causing formation abnormal spindle, which did not affect normal fibroblast NB1, Mrc-5 IBR3. For these reasons, could be good candidate chemopreventive or chemotherapeutic strategies.
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sci-hub.se 参考文章(38)
C Badie, J Bourhis, J Sobczak-Thépot, H Haddada, M Chiron, M Janicot, F Janot, T Tursz, G Vassal, p53-dependent G2 arrest associated with a decrease in cyclins A2 and B1 levels in a human carcinoma cell line. British Journal of Cancer. ,vol. 82, pp. 642- 650 ,(2000) , 10.1054/BJOC.1999.0976
Amanda Tivnan, Zaitun Zakaria, CaitrÃn O'Leary, Donat Kögel, Jenny L. Pokorny, Jann N. Sarkaria, Jochen H. M. Prehn, Inhibition of multidrug resistance protein 1 (MRP1) improves chemotherapy drug response in primary and recurrent glioblastoma multiforme. Frontiers in Neuroscience. ,vol. 9, pp. 218- 218 ,(2015) , 10.3389/FNINS.2015.00218
J. Martin Brown, Laura D. Attardi, The role of apoptosis in cancer development and treatment response Nature Reviews Cancer. ,vol. 5, pp. 231- 237 ,(2005) , 10.1038/NRC1560
Yujun George Zheng, Jiang Wu, Ziyue Chen, Masha Goodman, Chemical regulation of epigenetic modifications: opportunities for new cancer therapy. Medicinal Research Reviews. ,vol. 28, pp. 645- 687 ,(2008) , 10.1002/MED.20120
Mary Ann Jordan, Leslie Wilson, Microtubules as a target for anticancer drugs. Nature Reviews Cancer. ,vol. 4, pp. 253- 265 ,(2004) , 10.1038/NRC1317
B.A. Gilchrest, M.S. Eller, Cancer therapeutics: Smart and smarter Drugs of The Future. ,vol. 34, pp. 205- ,(2009) , 10.1358/DOF.2009.034.03.1336071
Adnan Erol, Deciphering the intricate regulatory mechanisms for the cellular choice between cell repair, apoptosis or senescence in response to damaging signals Cellular Signalling. ,vol. 23, pp. 1076- 1081 ,(2011) , 10.1016/J.CELLSIG.2010.11.023
Yonina R. Murciano-Goroff, Philanthropic partnerships and the future of cancer research Nature Reviews Cancer. ,vol. 15, pp. 125- 129 ,(2015) , 10.1038/NRC3862
Daniel B. Longley, D. Paul Harkin, Patrick G. Johnston, 5-Fluorouracil: mechanisms of action and clinical strategies Nature Reviews Cancer. ,vol. 3, pp. 330- 338 ,(2003) , 10.1038/NRC1074
Gérard A. Pinna, Gabriele Murineddu, Caterina Murruzzu, Valentina Zuco, Franco Zunino, Graziella Cappelletti, Roberto Artali, Giorgio Cignarella, Lucrezia Solano, Stefania Villa, Synthesis, modelling, and antimitotic properties of tricyclic systems characterised by a 2-(5-Phenyl-1H-pyrrol-3-yl)-1,3,4-oxadiazole moiety. ChemMedChem. ,vol. 4, pp. 998- 1009 ,(2009) , 10.1002/CMDC.200800428