期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 126, 期 -, 页码 218-224出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.09.094
关键词
Benzoisothiazoles; Piperazine; Isoxazole and cytotoxic activity
资金
- University with Potential for Excellence [14/4/2012(NS/PE)]
- University Grants Commission Government of India [f 4-1/2013(SAP II)]
- DOE [S0(22) 2013-2014/DOE-784]
- Central Tibetan Administration, Dharamasala
Synthesis of 3-(4((3-Pheny1-4,5-dihydroisoxazol-5-yl)methyl)piperazin-1-y1) benzoisothiazole derivatives (5a-i), which constitute a new class of isoxazolines, has been accomplished in regio-selective manner. These derivatives have been prepared by employing the reaction between substituted aldoximes (4a-i) and 3-(4-Allylpiperazin-1-yl) benzoisothiazole in presence of chloramine-T which afforded in good yields. These compounds were screened for cytotoxic activity on tumor cells. Four among the nine synthesized compounds were found to exhibit potent cytotoxic and antineoplastic activities in comparison to tumor necrosis factor-related apoptosis inducing ligand (TRAIL) protein in mammalian cancer cells. The rest of the derivatives showed moderate activity. (C) 2016 Published by Elsevier Masson SAS.
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