Abstract

Objective: The study was aimed to investigate the cytotoxic effect of S-5H-[1,2,4]-triazino (5,6-b) indol-3-yl-3,4-phenylethane-thioate derivatives as epidermal growth factor Receptor (EGFR) inhibitors.
 Methods: In the present study 14 novel triazine analogues were synthesized and characterized using different spectroscopic techniques such as FT-IR, NMR and Mass Spectroscopy. The anticancer activity was performed using MCF-7 (breast cancer) and K-562 (leukaemia) cell lines. Further, molecular docking was carried out using Vlife Molecular Docking Software (MDS) on crystal structure of epidermal growth factor receptor (EGFR) to identify the binding mode of interaction with an active site.
 Results: Compounds MA-7, MA-8, MA-12, MA-13 and MA-14 show potent activity against cancer cell lines in the range of<10 to 84.4 µg/ml. Further molecular docking on EGFR also supports that there is a strong correlation between in silico and in vitro biological activity. The results of this study may be further useful for lead optimization process.
 Conclusion: The results of this study indicates that the synthesized triazine analogues can give a potential lead as an anticancer agent.

Highlights

  • Cancer is a condition that refers to a state in which the cell present in the body gone awry and reproduced in an uncontrollable manner [1]

  • The other type of cancer we have focused is leukaemia which is known as blood cancer and starts with the bone marrow and results into the multiplication of white blood cells (WBCs) [9]

  • Sometimes some hairy thin projections are seen in an infrequent chronic leukaemia which is called as hairy cell leukaemia (HCL) that starts with the bone marrow and the accumulation of these hairy cells present in the bone marrow, liver and spleen

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Summary

Introduction

Cancer is a condition that refers to a state in which the cell present in the body gone awry and reproduced in an uncontrollable manner [1]. The healthy tissues and organs that are present in the body are proliferated or intrude get destroyed [2]. The symptom of cancer originated from the coercing, pulverizing and destroying the surrounding healthy cells and tissues [4]. Development of breast cancer is seen most commonly in the cells present in the inner linings of the milk ducts and the lobules, which are the major source for the supply of the milk in the ducts [7]. The other type of cancer we have focused is leukaemia which is known as blood cancer and starts with the bone marrow and results into the multiplication of white blood cells (WBCs) [9]. There are no clear symptoms for the development of HCL in the early stage

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