Synthesis and tumor inhibitory activity of novel coumarin analogs targeting angiogenesis and apoptosis

Eur J Med Chem. 2014 Mar 21:75:211-21. doi: 10.1016/j.ejmech.2014.01.050.

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

Affiliations

1 Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College (Autonomous), Kuvempu University, Shimoga 577203, Karnataka, India.
2 Department of Chemistry, Yuvaraja's College (Autonomous), University of Mysore, Mysore 570 005, Karnataka, India.
3 Department of Biochemistry, Yuvaraja's College (Autonomous), University of Mysore, Mysore 570 005, Karnataka, India.
4 Department of Chemistry, Yuvaraja's College (Autonomous), University of Mysore, Mysore 570 005, Karnataka, India. Electronic address: shaukathara@yahoo.co.in.

PMID: 24534537 DOI: 10.1016/j.ejmech.2014.01.050

Abstract

A sequence of coumarin analogs 5a-j was obtained by multi step synthesis from hydroxy benzophenones (1a-j). The in vitro antiproliferative effect of the title compounds was tested against Ehrlich ascites carcinoma (EAC) and Daltons lymphoma ascites (DLA) cell lines. Among the series, compound 5c with bromo group in the benzophenone moiety was endowed with excellent antiproliferative potency with significant IC50 value. Further, in vivo antitumor effect of compound 5c against murine EAC and solid DL tumor model system was evident by the extended survivality. The tumor inhibitory mechanism of compound 5c was due to the antiangiogenesis and promotion of Apoptosis. These results suggest possible applications of compound 5c which could be developed as a potent Anticancer drug in the near future.

Keywords

Antiangiogenic; Antitumor; Coumarin analogs; Proapoptotic.

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