Synthesis and biological evaluation of novel isoxazolines linked via piperazine to 2- benzoisothiazoles as potent apoptotic agents

Byrappa, S. and Harsha Raj, M. and Kungyal, Tenzin and Narayana, U. K. N. and Bharathi P. Salimath and Rai, K. M. Lokanatha (2017) Synthesis and biological evaluation of novel isoxazolines linked via piperazine to 2- benzoisothiazoles as potent apoptotic agents. European Journal of Medicinal Chemistry, 126. 218 - 224. ISSN 0223-5234

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Official URL: https://doi.org/10.1016/j.ejmech.2016.09.094

Abstract

Synthesis of 3-(4-((3-Phenyl-4,5-dihydroisoxazol-5-yl)methyl)piperazin-1-yl) 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.

Item Type: Article
Uncontrolled Keywords: Benzoisothiazoles, Piperazine, Isoxazole and cytotoxic activity
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: C Swapna Library Assistant
Date Deposited: 26 Jun 2019 05:18
Last Modified: 13 Jan 2023 11:00
URI: http://eprints.uni-mysore.ac.in/id/eprint/3848

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