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

Eur J Med Chem. 2014 Nov 24:87:274-83. doi: 10.1016/j.ejmech.2014.09.069.

T Prashanth ¹, Prabhu Thirusangu ², B R Vijay Avin ², V Lakshmi Ranganatha ³, B T Prabhakar ², Shaukath Ara Khanum ⁴

Affiliations

1 Department of Chemistry, Yuvaraja's College, University of Mysore, Mysore 570005, Karnataka, India; Department of Chemistry, The National Institute of Engineering, Manandavadi Road, Mysore 570008, Karnataka, India.
2 Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (A), Kuvempu University, Shimoga 577203, Karnataka, India.
3 Department of Chemistry, Yuvaraja's College, University of Mysore, Mysore 570005, Karnataka, India; PG Department of Chemistry, St. Philomena's College, Mysore, Bannimantap, Mysore 570015, India.
4 Department of Chemistry, Yuvaraja's College, University of Mysore, Mysore 570005, Karnataka, India. Electronic address: shaukathara@yahoo.co.in.

PMID: 25261825 DOI: 10.1016/j.ejmech.2014.09.069

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.

Keywords

Antiproliferation; Benzophenone; In vivo; Thiazoles; VEGF-A.

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