Enhancement of Anticancer Activity of N(4)1-(2-Pyridyl)piperazinyl 5-Nitroisatin Thiosemicarbazone on Chelation with Copper(II)

Narendra Kumar Singh1,, Smriti Shrestha2, Nerina Shahi2, Ravinder Kumar Choudhary3, Anupa A. Kumbhar4, Yuba Raj Pokharel2,* and Paras Nath Yadav5,*

1Department of Chemistry, Amrit Campus, Tribhuvan University, Kathmandu, Nepal

2Faculty of Life Science and Biotechnology, South Asian University, Akbar Bhawan, Chanakyapuri, New Delhi-110021, India

3Department of Chemistry, Gurukula Kangri Vishwavidyalaya, Haridwar-249404, India

4Department of Chemistry, Savitribai Phule Pune University, Pune-411007, India

5Central Department of Chemistry, Tribhuvan University, Kirtipur, Kathmandu, Nepal

*Corresponding authors: E-mail: yrp@sau.ac.in; pnyadav219@gmail.com

Abstract

5-Nitroisatin-4-(1-(2-pyridyl)piperazinyl)-3-thiosemicarbazone (Nitistpyrdlpz) and its Cu(II) complex were synthesized and characterized by CHN and thermal analysis and spectroscopic measurements viz. UV-vis, FTIR, 1H NMR, 13C NMR, ESI-HRMS, PXRD and EPR. In the complex, copper(II) ion is coordinated by terdentate thiosemicarbazone anion and one chloride ion in a distorted square planar geometry. The synthesized compounds against breast cancer cell lines; MCF-7 and MDA-MB-231 and epidermoid carcinoma; A431 showed that the complex contributed to reduce the percentage of cell viability toward all the tested cell lines but remarkable contribution toward MDA-MB-231 cell line. The IC50 of the complex and free ligand was found in the range of IC50 0.85-1.24 μM and IC50 3.28-3.53 μM, respectively. Among those cell lines, the complex may be the better anticancer agent toward MDA-MB-231 because of its action at micromolar concentration (IC50 0.85 μM).

Keywords

Anticancer activity, Copper(II) complex, MDA-MB-231 cell line, 5-Nitroisatin, Thiosemicarbazone.

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