Synthesis of novel morpholine conjugated benzophenone analogues and evaluation of antagonistic role against neoplastic development

Al-Ghorbani, Mohammed and Thirusangu, Prabhu and Gurupadaswamy, H. D. and Vigneshwaran, V. and Mohammed, Yasser H. E. and Prabhakar, B. T. and Khanum, Shaukath Ara (2017) Synthesis of novel morpholine conjugated benzophenone analogues and evaluation of antagonistic role against neoplastic development. Bioorganic Chemistry, 71. 55 - 66. ISSN 0045-2068

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Official URL: https://doi.org/10.1016/j.bioorg.2017.01.011

Abstract

A series of novel 4-benzyl-morpholine-2-carboxylic acid N′-2-(4-benzoyl-phenoxy)-acetyl-hydrazide derivatives 8a-j has been synthesized from (4-hydroxy-aryl)-aryl methanones through a multi-step reaction sequence and then evaluated for anti-proliferative activity in vitro against various types of neoplastic cells of mouse and human such as DLA, EAC, MCF-7 and A549 cells. From the cytotoxic studies and structural activity relationship of compounds 8a-j, it is clear that methyl group on the B ring of benzophenone is essential for antiproliferative activity and bromo at ortho position (compound 8b) and methyl at para position (compound 8f) on A ring of benzophenone are significant for extensive anti-mitogenic activity. Investigation on clonogenesis and Fluorescence-activated cell sorting suggests that compounds 8b and 8f have the potency to exhibit the prolonged activity with cell cycle arrest on G2/M phase against cancer progression. Further, the compounds 8b and 8f inhibit murine ascites lymphoma through caspase activated DNase mediated apoptosis.

Item Type: Article
Uncontrolled Keywords: Benzophenone, Morpholine, CAD, DLA, MCF-7
Subjects: C Chemical Science > Chemistry
Divisions: Yuvaraj college > Chemistry
Depositing User: MUL SWAPNA user
Date Deposited: 24 Jun 2019 10:30
Last Modified: 24 Jun 2019 10:30
URI: http://eprints.uni-mysore.ac.in/id/eprint/3752

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