Synthesis of oxadiazole-morpholine derivatives and manifestation of the repressed CD31 Microvessel Density (MVD) as tumoral angiogenic parameters in Dalton's Lymphoma

Al-Ghorbani, M. and Vigneshwaran, V. and Ranganatha, V. L. and Prabhakar, B. T. and Khanum, S. A. (2015) Synthesis of oxadiazole-morpholine derivatives and manifestation of the repressed CD31 Microvessel Density (MVD) as tumoral angiogenic parameters in Dalton's Lymphoma. BIOORGANIC CHEMISTRY, 60. pp. 136-146. ISSN 1090-2120

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Official URL: https://doi.org/10.1016/j.bioorg.2015.04.008

Abstract

A series of oxadiazole derivatives possessing morpholine 6a-l were synthesized by nucleophilic substitution reaction of key intermediates 1,3,4]-oxadiazole-2-thiol derivatives 5a-l with 4-(2-chloroethyl) morpholine. Compounds 6a-l were evaluated for their in vitro and in vivo antitumor potential in Dalton's Lymphoma Ascites (DLA) tumor cells. Among 6a-l series, compound 6a with concentration similar to 8.5 mu M have shown extensive cytotoxicity in vitro and 85% reduction in tumor volume in vivo, attributing an excellent anti-proliferative capability towards the cancer cells. Compound 6a has extensively inhibited the Microvessel Density (MVD) or tumoral neovasculature which was evident from the CD31 immuno staining and peritoneal H&E staining. The major reason for the antiproliferative activity of compound 6a was due to the repression of tumor vasculature. (C) 2015 Published by Elsevier Inc.

Item Type: Article
Uncontrolled Keywords: Oxadiazole-morpholine; Microvessel Density (MVD); CD31; Angiogenesis; Dalton's Lymphoma
Subjects: C Chemical Science > Chemistry
Divisions: Yuvaraj college > Chemistry
Depositing User: Shrirekha N
Date Deposited: 06 Jun 2019 06:02
Last Modified: 06 Jun 2019 06:02
URI: http://eprints.uni-mysore.ac.in/id/eprint/2659

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