Synthesis of novel morpholine conjugated benzophenone analogues and evaluation of antagonistic role against neoplastic development.
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| 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.
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| Authors | Mohammed Al-Ghorbani, Prabhu Thirusangu, H D Gurupadaswamy, V Vigneshwaran, Yasser H E Mohammed, B T Prabhakar, Shaukath Ara Khanum |
| Journal | Bioorganic chemistry (Bioorg Chem) Vol. 71 Pg. 55-66 (04 2017) ISSN: 1090-2120 [Electronic] United States |
| PMID | 28139247 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't) |
| Copyright | Copyright © 2017 Elsevier Inc. All rights reserved. |
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