Synthesis and evaluation of novel benzophenone-thiazole derivatives as potent VEGF-A inhibitors

Prashanth, T. and Thirusangu, P. and Vijay Avin, B. R. and Lakshmi Ranganatha, V. and Prabhakar, B. T. and Khanum, S. A. (2014) Synthesis and evaluation of novel benzophenone-thiazole derivatives as potent VEGF-A inhibitors. European Journal of Medicinal Chemistry, 87. pp. 274-283. ISSN 0223-5234

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Abstract

A series of 2-(4-benzoyl-phenoxy)-N-(4-phenyl-thiazol-2-yl)-Acetamides (10a-n) were synthesized by multistep reaction sequence and all the compounds were well characterized for structural elucidation. The in vitro cytotoxicity of compounds 10a-n was evaluated against EAC and DLA cell lines using trypan blue dye exclusion method. Further MTT assay and LDH release assay, followed by in vivo studies on murine model were also evaluated. The compound 10h with a methyl and fluoro groups at benzophenone moiety and methoxy group at phenyl ring was in a leading position to exhibit the promising antiproliferative effect through translational VEGF-A inhibition.

Item Type:	Article
Uncontrolled Keywords:	animal experiment, animal model, antiproliferative activity, Article, controlled study, drug cytotoxicity, drug potency, human, in vitro study, in vivo study, mouse, nonhuman, structure activity relation, unclassified drug, animal, Animals, Cell Line, chemistry, drug screening, Humans, Structure-Activity Relationship, synthesis, Tumor, tumor cell line, animal cell, male, Male, antagonists and inhibitors, drug design, Drug Design, MTT assay, Chemistry Techniques, Synthetic, evaluation study, benzophenone, benzophenone derivative, Benzophenones, lactate dehydrogenase, Mice, RNA, Disease Progression, methyl group, thiazole derivative, Thiazoles, Vascular Endothelial Growth Factor A, vasculotropin A, Xenograft Model Antitumor Assays, disease course, 2 (4 benzoyl 2, 2 (4 benzoyl 2 bromo phenoxy) n (4 phenyl thiazol 2 yl) acetamide, 2 (4 benzoyl 2 methyl phenoxy) n (4 phenyl thiazol 2yl) acetamide, 2 (4 benzoyl 2 methyl phenoxy) n 4 (4 methoxy phenyl) thiazol 2 yl acetamide, 2 2 methyl 4 (2 methyl benzoyl) phenoxy n (4 phenyl thiazol 2 yl) acetamide, 2 2 methyl 4 (4 methyl benzoyl) phenoxy n (4 phenyl thiazol 2 yl) acetamide, 2 4 (2 fluoro benzoyl) 2 methyl phenoxy n (4 phenylthiazol 2 yl) acetamide, 2 4 (3 bromo benzoyl) 2 methyl phenoxy n (4 phenylthiazol 2 yl) acetamide, 2 4 (3 bromo benzoyl) 2 methyl phenoxy n 4 (4 methoxy phenyl) thiazol 2 yl acetamide, 2 4 (3 fluoro benzoyl) 2 methyl phenoxy n 4 (4 methoxy phenyl) thiazol 2 yl acetamide, 2 4 (4 fluoro benzoyl) 2 methyl phenoxy n 4 (4 methoxy phenyl) thiazol 2 yl acetamide, 2 4 (4 fluoro-benzoyl) 2 methyl phenoxy n (4 phenylthiazol 2 yl) acetamide, 6 dimethyl phenoxy) n (4 phenyl thiazol 2 yl) acetamide, 6 dimethyl phenoxy) n 4 (4 methoxyphenyl) thiazol 2 yl acetamide, drug inhibition, trypan blue, vasculotropin inhibitor
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Arshiya Kousar Library Assistant
Date Deposited:	31 Aug 2019 10:06
Last Modified:	31 Aug 2019 10:06
URI:	http://eprints.uni-mysore.ac.in/id/eprint/4282

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