Design, docking and crystal structure determination of copper based chemotherapeutic as potential topoisomerase inhibitor: In vitro DNA binding, nuclease studies, in vitro and in vivo anticancer activity

3^rd World Congress on Cancer Science & Therapy

October 21-23, 2013 DoubleTree by Hilton Hotel San Francisco Airport, CA, USA

Sartaj Tabassum

Accepted Abstracts: J Cancer Sci Ther

Abstract :

Small molecules that bind to DNA minor groove region which inhibit the expression of DNA-processing enzymes (topoisomerase I and II) and its delivery towards the targeted cell via binding to carrier protein represent an important class of anticancer drugs. In this point of view, a mononuclear and di nuclear Cu(II), Sn(IV), Ru(III) complexes were designed and synthesized and characterized by elemental analysis, spectroscopic and magnetic studies. The structure of complexes were solved by single crystal X-ray diffraction method which revealed that Cu(II) metal ion arranged in a N 4 O coordination environment showing distorted square pyramidal geometry. The complexes were successively docked towards the molecular target DNA, HSA and topoisomerase in a site selective manner and further validated by in vitro DNA and employing different biophysical techniques. The pBR322 DNA cleavage and topoisomerase relaxation assay was investigated using concentration dependent agarose gel electrophoresis. In vitro and in vivo anticancer activity was performed.

Biography :

Sartaj Tabassum is working as Professor in the Department of Chemistry, Aligarh Muslim University, Aligarh. He has published 86 papers in the journals of international repute. He is life member of ACS (USA) ICC, CRSI, ISCB, DNA Society of India and American Nano Society(USA). He has successfully completed many research schemes granted by TWAS, Italy, CSIR, New Delhi, DBT, Government of India. As a distinguished scientist, he was awarded Overseas Associateship award in 2005 by DBT, Goverment of India. He has signed several MoU and joint research collaboration with University of Camerino UNICAM, Italy, USM Malaysia and USTC, China.